Tag: 400-500

The author of 《Intracellular Notch1 Signaling in Cancer-Associated Fibroblasts Dictates the Plasticity and Stemness of Melanoma Stem/Initiating Cells》 were Du, Yan; Shao, Hongwei; Moller, Mecker; Prokupets, Rochelle; Tse, Yee Ting; Liu, Zhao-Jun. And the article was published in Stem Cells (Durham, NC, United States) in 2019. Product Details of 106685-40-9 The author mentioned the following in the article:

Cancer stem cells (CSCs) play critical roles in cancer initiation, metastasis, recurrence, and drug resistance. Recent studies have revealed involvement of cancer-associated fibroblasts (CAFs) in regulating CSCs. However, the intracellular mol. mechanisms that determine the regulatory role of CAFs in modulating the plasticity of CSCs remain unknown. Here, we uncovered that intracellular Notch1 signaling in CAFs serves as a mol. switch, which modulates tumor heterogeneity and aggressiveness by inversely controlling stromal regulation of the plasticity and stemness of CSCs. Using mesenchymal stem cell-derived fibroblasts (MSC-DF) harboring reciprocal loss-of-function and gain-of-function Notch1 signaling, we found that MSC-DFNotch1-/- prompted cocultured melanoma cells to form more spheroids and acquire the phenotype (CD271+ and Nestin+) of melanoma stem/initiating cells (MICs), whereas MSC-DFN1IC+/+ suppressed melanoma cell sphere formation and mitigated properties of MICs. Our data demonstrate that intracellular Notch1 signaling in CAFs is a mol. switch dictating the plasticity and stemness of MICs, thereby regulating melanoma aggressiveness, and therefore that targeting the intracellular Notch1 signaling pathway in CAFs may present a new therapeutic strategy for melanoma. The amounts of CD271+ MIC regulated by MSC-DF carrying high or low Notch1 pathway activity is well correlated with capability of melanoma metastasis, supporting that melanoma metastasis is MIC-mediated. Consistently, when cografted with melanoma cells into NOD scid gamma (NSG) mice, MSC-DFNotch1-/- increased, but MSC-DFN1IC+/+ decreased, the amounts of CD271+ MIC in melanoma tissue. MSC-DFNotch1-/- increased stemness of CD271+ MIC, which resultantly exhibited stronger aggressiveness in vitro and in vivo, by upregulating Sox2/Oct4/Nanog expression. In the part of experimental materials, we found many familiar compounds, such as 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9Product Details of 106685-40-9)

6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas:106685-40-9) is a third-generation synthetic retinoid and a highly lipophilic compound derived from naphthoic acid. It is widely used in the treatment of acne.Product Details of 106685-40-9

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《Selective RAR agonists for acne vulgaris: A narrative review.》 was published in Journal of cosmetic dermatology in 2020. These research results belong to Kassir, Martin; Karagaiah, Priyanka; Sonthalia, Sidharth; Katsambas, Andreas; Galadari, Hassan; Gupta, Mrinal; Lotti, Torello; Wollina, Uwe; Abdelmaksoud, Ayman; Grabbe, Stephan; Goldust, Mohamad. Safety of 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid The article mentions the following:

BACKGROUND: Acne vulgaris is a chronic disfiguring inflammatory disease of adolescents and adults affecting up to 90% of the population around the world. The sequence of etiopathogenesis in acne is not completely understood but involves abnormalities in sebum production, follicular plugging, proliferation of propionibacterium acnes, and chronic inflammation. AIMS: This review aims to summarize the features of the topical selective RAR agonists in treating acne vulgaris with a special emphasis on the 4th generation topical retinoid trifarotene. METHODS: Studies were identified by searching electronic databases (MEDLINE and PubMed) till August 2019 and reference lists of respective articles. Only articles published in English language were included. RESULTS: Topical retinoids have been first line of treatment for more than 30 years now in treating mild to moderate acne vulgaris. Third generation retinoids like adapalene and tazarotene are selective RAR and γ agonists, having an additional anti-inflammatory action along with their comedolytic effects and work well in combinations with topical antibiotics, due to the stability of chemical composition. CONCLUSION: Trifarotene is a new 4th generation retinoid with selective action on RAR-γ receptor alone, which is specific for skin, and it is safe for long-term maintenance therapy with good efficacy and tolerability.6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9Safety of 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid) was used in this study.

6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas:106685-40-9) may be used as a pharmaceutical reference standard for the quantification of the analyte in topical gel formulations using high-performance liquid chromatography technique.Safety of 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid

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SDS of cas: 106685-40-9In 2020 ,《Ion Pair Strategy in Solid Lipid Nanoparticles: a Targeted Approach to Improve Epidermal Targeting with Controlled Adapalene Release, Resulting Reduced Skin Irritation》 was published in Pharmaceutical Research. The article was written by Rodrigues, Linna B. O.; Lima, Flavia A.; Alves, Camila P. B.; Martins-Santos, Elisangela; Aguiar, Marta M. G.; Oliveira, Cleida A.; Orefice, Rodrigo L.; Ferreira, Lucas A. M.; Goulart, Gisele A. C.. The article contains the following contents:

Abstract: Purpose: Adapalene (AD) is one of the main retinoids used in the topical therapy of acne, an extremely common skin disease usually associated with psychol. morbidity. However, like other retinoids, AD is frequently associated with skin irritation. To overcome the skin irritation, we proposed the encapsulation of AD in solid lipid nanoparticles (SLNs) using the ion pair strategy. Methods: The developed SLN-AD was characterized by high-performance liquid chromatog., differential scanning calorimetry, X-ray diffraction, synchrotron small-angle X-ray scattering, and transmission electron microscopy. In vitro permeation tests using porcine skin and in vivo mice skin irritation test were performed to evaluate, resp., the drug’s skin distribution and the skin irritation. Results: The characterization studies were able to demonstrate that the proposed strategy effectively provided high AD encapsulation in SLNs and its incorporation into a hydrophilic gel. Sustained release, epidermal targeting, and less skin irritation were observed for SLN-AD gel in comparison to the marketed AD gel. Conclusions: The studies demonstrated that the encapsulation of AD in SLNs through the formation of an ion pair is a valuable alternative to diminish the adverse skin reactions caused by AD and can optimize patient adherence to treatment. In the experiment, the researchers used 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9SDS of cas: 106685-40-9)

6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas:106685-40-9) is a third-generation synthetic retinoid and a highly lipophilic compound derived from naphthoic acid. It is widely used in the treatment of acne.SDS of cas: 106685-40-9

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In 2019,Journal of Drugs in Dermatology included an article by Kircik, Leon H.. Product Details of 106685-40-9. The article was titled 《Anti-inflammatory dose doxycycline plus adapalene 0.3% and benzoyl peroxide 2.5% Gel for severe acne》. The information in the text is summarized as follows:

Acne is primarily an inflammatory disease. Anti-inflammatory dose doxycycline (40mg: 30mg immediate release and 10mg delayed release beads) is approved for the treatment of rosacea but with demonstrated efficacy for acne. Fixed combination adapalene C.3% and benzoyl peroxide 2.5% gel is a once-daily formulation approved for the topical management of acne vulgaris. It has both antiinflammatory and anti-comedogenic properties. Options for management of severe acne are somewhat limited; many patients are not candidates for or refuse treatment with isotretinoin. Systemic antibiotics may be indicated; acne treatment guidelines emphasize antibiotic stewardship in light of increasing concerns about antibiotic resistance and call for the judicious use of conventional systemic antibiotics. This single-center, open label pilot study involving 20 subjects with severe acne assessed the effects of combination treatment using anti-inflammatory dose doxycycline plus adapalene 0.3% and benzoyl peroxide 2.5% gel on IGA scores as well as inflammatory lesion, non-inflammatory lesion, and nodule counts. By week 12, 95% of subjects had at least a 2-grade improvement in IGA scores. Reductions in inflammatory and non-inflammatory lesion counts were statistically significant beginning at week 4 and continuing through week 12. By week 4, the percentage of patients with O nodules was 70%, compared to baseline of 20%. Further improvements were seen through week 12. Treatment was welltolerated with no serious treatment-related adverse events. Combination treatment with anti-inflammatory dose doxycycline plus combination adapalene 0.3% and benzoyl peroxide 2.5% gel is safe and effective for management of severe acne. In the experiment, the researchers used many compounds, for example, 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9Product Details of 106685-40-9)

6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas:106685-40-9) is a third-generation synthetic retinoid and a highly lipophilic compound derived from naphthoic acid. It is widely used in the treatment of acne.Product Details of 106685-40-9

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

《First reported cases of actinic folliculitis treated successfully with topical retinoid.》 was published in Clinical and experimental dermatology in 2020. These research results belong to Rahman, S; Powell, J; Al-Ismail, D. Application of 106685-40-9 The article mentions the following:

Actinic folliculitis (AF) is a rare recurrent seasonal photodermatosis, relatively newly characterized by nonpruritic, monomorphic pustules and papules appearing 4-24 h after exposure to sunlight. Lesions usually affect the face but also appear on the upper chest and arms. Resolution normally occurs within 7-10 days with cessation of sunlight exposure. AF is resistant to standard treatments used for acne vulgaris and acne rosacea, with only oral retinoids previously being reported as effective. We report the first two cases, to our knowledge, of AF responding extremely effectively to a topical retinoid. After reading the article, we found that the author used 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9Application of 106685-40-9)

6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas:106685-40-9) may be used as a pharmaceutical reference standard for the quantification of the analyte in topical gel formulations using high-performance liquid chromatography technique.Application of 106685-40-9

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Synthetic Route of C28H28O3In 2020 ,《The third-generation retinoid adapalene triggered DNA damage to induce S-phase arrest in HaCat cells》 appeared in Fundamental & Clinical Pharmacology. The author of the article were Wang, Cheng; Li, Hongyang; Ma, Pengcheng; Sun, Jianfang; Li, Lingjun; Wei, Jun; Tao, Lei; Qian, Kun. The article conveys some information:

Epidermal proliferative diseases consisted of a series of common skin diseases, most of which were recurrent chronic skin diseases, and had greatly neg. influence on the life quality of patient. Retinoids exhibited vital roles in the treatment of many skin diseases. Our recent study demonstrated that adapalene significantly inhibited the growth of HaCat cells, and the inhibitory activity was stronger than other retinoids, such as all-trans-retinoic acid, acitretin, isotretinoin, tazarotene, and bexarotene. Further study showed that adapalene suppressed the colony formation of HaCat cells, and it dramatically triggered S-phase arrest and apoptosis, rather than G1 phase arrest which was reported in other retinoids in several studies. Addnl., adapalene treatment greatly upregulated the protein expression of DNA damage marker γ-H2AX, which was in accord with the results of the elongation of tail moment by comet electrophoresis anal. Moreover, DNA damage was triggered and DNA repair was suppressed synchronously with adapalene treatment, which accounted for the mechanism of S-phase arrest induced by adapalene. In summary, our recent work demonstrated that adapalene showed strong anti-proliferation activity in HaCat cells and could be an alternative agent for the epidermal proliferative disease. In the experiment, the researchers used many compounds, for example, 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9Synthetic Route of C28H28O3)

6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas:106685-40-9) is a third-generation synthetic retinoid and a highly lipophilic compound derived from naphthoic acid. It is widely used in the treatment of acne.Synthetic Route of C28H28O3

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Ether – Wikipedia,
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In 2019,Journal of Dermatological Treatment included an article by Chlebus, Ewa; Serafin, Monika; Chlebus, Marcin. Category: ethers-buliding-blocks. The article was titled 《Is maintenance treatment in adult acne important Benefits from maintenance therapy with adapalene, and low doses of alpha and beta hydroxy acids》. The information in the text is summarized as follows:

Adult acne is a chronic disease with uncontrolled exacerbations, associated with a psychol. burden of the patient and medical expenses. The aim of the study was to check the efficacy of maintenance therapy of adult acne. It is essential part of treatment as adult acne usually has a long-lasting and recurring course. In the study, the efficacy of maintenance therapy in patients with adult acne is evaluated. In this study, 100 patients (aged 25-39 years of age) with mild and moderate adult acne were enrolled. The maintenance therapy (adapalene 0.1% three times a week and low doses of alpha and beta hydroxy acids) led to a significant decrease in the number of acne lesions (from 31.3 to 12.25; p < .001) and severity of seborrhea (p < .001). Maintenance therapy brings significant improvements in the reduction of non-inflammatory and inflammatory lesions in patients with mild and moderate adult acne. In the experiment, the researchers used 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9Category: ethers-buliding-blocks)

6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas:106685-40-9) may be used as a pharmaceutical reference standard for the quantification of the analyte in topical gel formulations using high-performance liquid chromatography technique.Category: ethers-buliding-blocks

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In 2019,Upsala journal of medical sciences included an article by Brboric, Anja; Vasylovska, Svitlana; Saarimäki-Vire, Jonna; Espes, Daniel; Caballero-Corbalan, José; Larfors, Gunnar; Otonkoski, Timo; Lau, Joey. Category: ethers-buliding-blocks. The article was titled 《Characterization of neural crest-derived stem cells isolated from human bone marrow for improvement of transplanted islet function.》. The information in the text is summarized as follows:

Background: Murine boundary cap-derived neural crest stem cells (NCSCs) are capable of enhancing islet function by stimulating beta cell proliferation as well as increasing the neural and vascular density in the islets both in vitro and in vivo. This study aimed to isolate NCSC-like cells from human bone marrow.Methods: CD271 magnetic cell separation and culture techniques were used to purify a NCSC-enriched population of human bone marrow. Analyses of the CD271+ and CD271- fractions in terms of protein expression were performed, and the capacity of the CD271+ bone marrow cells to form 3-dimensional spheres when grown under non-adherent conditions was also investigated. Moreover, the NCSC characteristics of the CD271+ cells were evaluated by their ability to migrate toward human islets as well as human islet-like cell clusters (ICC) derived from pluripotent stem cells.Results: The CD271+ bone marrow population fulfilled the criterion of being multipotent stem cells, having the potential to differentiate into glial cells, neurons as well as myofibroblasts in vitro. They had the capacity to form 3-dimensional spheres as well as an ability to migrate toward human islets, further supporting their NCSC identity. Additionally, we demonstrated similar migration features toward stem cell-derived ICC.Conclusion: The results support the NCSC identity of the CD271-enriched human bone marrow population. It remains to investigate whether the human bone marrow-derived NCSCs have the ability to improve transplantation efficacy of not only human islets but stem cell-derived ICC as well. In the experiment, the researchers used 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9Category: ethers-buliding-blocks)

6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas:106685-40-9) may be used as a pharmaceutical reference standard for the quantification of the analyte in topical gel formulations using high-performance liquid chromatography technique.Category: ethers-buliding-blocks

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Jiang, Guangcheng; Stalewski, Jacek; Galyean, Robert; Dykert, John; Schteingart, Claudio; Broqua, Pierre; Aebi, Audrey; Aubert, Michel L.; Semple, Graeme; Robson, Peter; Akinsanya, Karen; Haigh, Robert; Riviere, Pierre; Trojnar, Jerzy; Junien, Jean Louis; Rivier, Jean E. published an article on February 1 ,2001. The article was titled 《GnRH Antagonists: A New Generation of Long Acting Analogues Incorporating p-Ureido-phenylalanines at Positions 5 and 6》, and you may find the article in Journal of Medicinal Chemistry.HPLC of Formula: 324017-21-2 The information in the text is summarized as follows:

A series of antagonists of gonadotropin-releasing hormone (GnRH) of the general formula Ac-D2Nal-D4Cpa-D3Pal-Ser-4Aph/4Amf(P)-D4Aph/D4Amf(Q)-Leu-ILys-Pro-DAla-NH2 was synthesized, characterized, and screened for duration of inhibition of LH release in a castrated male rat assay. Selected analogs were tested in a reporter gene assay (IC50 and pA2) and an in vitro histamine release assay. P and Q contain urea/carbamoyl functionalities designed to increase potential intra- and intermol. hydrogen bonding opportunities for structural stabilization and peptide/receptor interactions, resp. These substitutions resulted in analogs with increased hydrophilicity and a lesser propensity to form gels in aqueous solution than azaline B [Ac-D2Nal-D4Cpa-D3Pal-Ser-4Aph(Atz)-D4Aph(Atz)-Leu-ILys-Pro-DAla-NH2; Atz = 3′-amino-1H-1′,2′,4′-triazol-5′-yl], and in some cases they resulted in a significant increase in duration of action after s.c. administration. Ac-D2Nal-D4Cpa-D3Pal-Ser-4Aph(L-hydroorotyl)-D4Aph(carbamoyl)-Leu-ILys-Pro-DAla-NH2 (acetate salt is FE200486) (I) and eight other congeners (20, 35, 37, 39, 41, 45-47) were identified that exhibited significantly longer duration of action than acyline [Ac-D2Nal-D4Cpa-D3Pal-Ser-4Aph(Ac)-D4Aph(Ac)-Leu-ILys-Pro-DAla-NH2] (6) when administered s.c. in castrated male rats at a dose of 50 μg in 100 μL of phosphate buffer. No correlation was found between retention times on a C18 reverse phase column using a triethylammonium phosphate buffer at pH 7.0 (a measure of hydrophilicity) or affinity in an in vitro human GnRH report gene assay (pA2) and duration of action. I was selected for preclin. studies, and some of its properties were compared to those of other clin. candidates. In the intact rat, ganirelix, abarelix, azaline B, and I inhibited plasma testosterone for 1, 1, 14, and 57 days, resp., at 2 mg/kg s.c. in 5% mannitol (injection volume = 20 μL). Based on the information that I, 33, 35 and 37 were significantly shorter acting than acyline or azaline B after i.v. administration (100 μg/rat), we surmised that the very long duration of action of the related I (for example) was likely due to unique physicochem. properties such as solubility in aqueous milieu, comparatively low propensity to form gels, and ability to diffuse at high concentrations in a manner similar to that described for slow release formulations of peptides. Indeed, in rats injected s.c. with I (2 mg/kg), plasmatic concentrations of I remained above 5 ng/mL until day 41, and the time after which they dropped below 3 ng/mL and plasma LH levels started rising until full recovery was reached at day 84 with levels of I hovering around 1 ng/mL. Addnl., I was less potent at releasing histamine from isolated rat mast cells than any of the GnRH antagonists presently described in preclin. reports. In the experiment, the researchers used many compounds, for example, Fmoc-D-Phe(4-NH2)-OH(cas: 324017-21-2HPLC of Formula: 324017-21-2)

Fmoc-D-Phe(4-NH2)-OH(cas: 324017-21-2) belongs to ethers.HPLC of Formula: 324017-21-2Although ethers resist hydrolysis, they are cleaved by hydrobromic acid and hydroiodic acid. Hydrogen chloride cleaves ethers only slowly.

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Ether – Wikipedia,
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《Adverse events related to topical drug treatments for acne vulgaris》 was published in Expert Opinion on Drug Safety in 2020. These research results belong to Otlewska, Agnieszka; Baran, Wojciech; Batycka-Baran, Aleksandra. Application In Synthesis of 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid The article mentions the following:

A review. : Acne vulgaris is a widespread skin disease. Topical therapy is a standard treatment for mild to moderate acne. Given the complex pathophysiol. of acne, various agents with complementary action are nowadays frequently combined to increase the efficacy of therapy.: This review focus on safety profile of topical agents used for the treatment of acne vulgaris, including topical retinoids, benzyl peroxide, azelaic acid, topical antibiotic, and combined agents. Data from clin. trials but also metanalyses, systematic reviews, and other secondary analyses are presented.: In general, topical agents used for acne vulgaris have a favorable safety profile. The most commonly reported AEs were associated with local skin irritation, usually mild to moderate in intensity, intermittent, and rarely led to the cessation of therapy. Irritative potential seems to be highest for BPO and topical retinoids. Due to the possibility of development of Cutibacterium acnes resistance, topical antibiotics should not be used in monotherapy but as a part of combination therapy. In female adolescent and adults of childbearing potential, topical retinoids should be used with caution, because they are contraindicated in pregnant females (FDA Pregnancy category) C (adapalene, tretinoin) and X (tazarotene). In addition to this study using 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid, there are many other studies that have used 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9Application In Synthesis of 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid) was used in this study.

6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas:106685-40-9) is a third-generation synthetic retinoid and a highly lipophilic compound derived from naphthoic acid. It is widely used in the treatment of acne.Application In Synthesis of 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem