Tag: 400-500

Feng, Siliang; Li, Senhao; Kang, Xiaoyu; Liu, Keliang published an article in Journal of Chemical Research. The title of the article was 《One step synthesis of biotinylated amino acids》.COA of Formula: C24H22N2O4 The author mentioned the following in the article:

A rapid method is reported for the preparation of biotinylated 4-amino-D-phenylalanine(D-Aph) with Fmoc (Fmoc = 9-fluorenylmethoxycarbonyl) as the protecting group at the α-amino. Different coupling reagents and conditions were studied to get the biotinylated compound Coupling reagents like 1-[bis(dimethylamino)methylene]-1H-benzotriazolium 3-oxide hexafluorophosphate and BOP were found to be very efficient. Biotinylated Boc-L-Aph and biotinylated Fmoc-L-lysine were also successfully prepared by this method. In the part of experimental materials, we found many familiar compounds, such as Fmoc-D-Phe(4-NH2)-OH(cas: 324017-21-2COA of Formula: C24H22N2O4)

Fmoc-D-Phe(4-NH2)-OH(cas: 324017-21-2) belongs to ethers.Ethers do have nonbonding electron pairs on their oxygen atoms, and they can form hydrogen bonds with other molecules (alcohols, amines, etc.) that have O―H or N―H bonds. COA of Formula: C24H22N2O4 The ability to form hydrogen bonds with other compounds makes ethers particularly good solvents for a wide variety of organic compounds and a surprisingly large number of inorganic compounds.

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

Abdel-Wahab, Hossam M.; Ali, Amira K.; Ragaie, Maha Hussain published an article in 2022. The article was titled 《Calcipotriol: A novel tool in treatment of acne vulgaris》, and you may find the article in Dermatologic Therapy.Name: 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid The information in the text is summarized as follows:

Retinoids and active vitamin D3 analogs regulate the proliferation and differentiation of keratinocytes. Retinoids are the main stay in the treatment of acne vulgaris through their comedolytic and anti-inflammatory effects. However, the effect of calcipotriol on the different forms of acne lesions has not been reported. This split face prospective study aimed to detect the efficacy of topical calcipotriol in the treatment of acne lesions in comparison with that of adapalene. Forty patients with acne vulgaris were treated with topical calcipotriol (0.005%) cream and 0.1% adapalene gel on the right and left sides of the face resp. Clin. and histol. assessment of the used treatments was done 2 mo after the start of treatment. Two months after treatment, there was significant reduction of all acne lesions with significant decrease of physician global assessment and patient global assessment scores (p = 0.0001) on both sides of the face with no significant difference between both sides. Histol., there was significant decrease in the d. of inflammatory infiltrate, which was more significant on the right side (p < 0.0001). Topical calcipotriol can serve a significant role in the treatment of acne vulgaris, through its anti-inflammatory effect which was comparable to that of adapalene. 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: 106685-40-9Name: 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.Name: 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid

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

Lee, Na Hyun; Choi, Mi Jin; Yu, Hana; Kim, Jea Il; Cheon, Hyae Gyeong published an article in 2022. The article was titled 《Adapalene induces adipose browning through the RARβ-p38 MAPK-ATF2 pathway》, and you may find the article in Archives of Pharmacal Research.HPLC of Formula: 106685-40-9 The information in the text is summarized as follows:

Abstract: Adipose browning has recently been reported to be a novel therapeutic strategy for obesity. Because the retinoic acid receptor (RAR) is a potential target involved in browning, adapalene (AD), an anti-acne agent with RAR agonism, was examined in detail for its effects on adipose browning and the underlying mechanisms in vitro and in vivo. AD upregulated the expression of adipose browning-related markers in a concentration-dependent manner, promoted mitochondrial biogenesis, increased oxygen consumption rates, and lowered lipid droplet sizes in differentiated 3T3/L1 white adipocytes. Among the three retinoic acid receptors (RARα, RARβ, and RARγ), knockdown of the gene encoding RARβ mitigated AD-induced adipose browning. Similarly, LE135 (a selective RARβ antagonist) attenuated AD action, suggesting that AD promotes adipose browning through RARβ. Sequential phosphorylation of p38 mitogen-activated protein kinase (MAPK) and activating transcription factor 2 (ATF2) was critical for AD-induced adipose browning, based on the observations that either SB203580 (a p38 MAPK inhibitor) or ATF2 siRNA reduced the effects of AD. In vivo browning effects of AD were confirmed in C57BL/6J mice and high-fat diet-induced obese (DIO) mice after oral administration of AD either acutely or chronically. This study identifies new actions of AD as an adipose browning agent and demonstrates that RARβ activation followed by increased phosphorylation of p38 MAPK and ATF2 appears to be a key mechanism of AD action. In the experimental materials used by the author, we found 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9HPLC of Formula: 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.HPLC of Formula: 106685-40-9

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

《Trifarotene for the Treatment of Facial and Truncal Acne》 was written by Bell, Katheryn A.; Brumfiel, Caitlin M.; Haidari, Wasim; Boger, Laura. HPLC of Formula: 106685-40-9This research focused ontrifarotene treatment facial truncal acne; acne vulgaris; facial acne; retinoid; trifarotene; truncal acne. The article conveys some information:

This article reviews clin. trials to assess the efficacy, safety, and clin. application of trifarotene 0.005% cream (Aklief). A systematic review of the literature was performed using the terms trifarotene OR Aklief OR CD5789 in MEDLINE (PubMed) and EMBASE databases. Articles prior to May 2020 were considered for inclusion. Bibliogs. and ClinicalTrials.gov were also searched to identify further studies. Relevant English language and human studies related to pharmacol., clin. trials, and safety were considered. In the 52-wk phase III trial, treatment success rates for facial acne (Investigator Global Assessment [IGA] rating of no or almost no acne) and truncal acne (Physicianprimes Global Assessment [PGA] rating of no or almost no acne) were 65.1% and 66.9%, resp. Overall success rates (IGA and PGA success in the same patient) were 57.9%; 52.8% of patients had a Dermatol. Quality of Life Index score of 0 or 1, compared with 22.6% at baseline. Trifarotene was well tolerated, with pruritus, irritation, and sunburn as the most common adverse effects. Trifarotene is a newly Food and Drug Administration-labeled fourth-generation topical retinoid that shows particular promise in the treatment of facial and truncal acne vulgaris. It is an effective and safe addition to currently available retinoids. Trifarotene is effective and safe for treatment of facial and truncal acne. Future trials should compare its efficacy and tolerability with that of the older, clin. established retinoids. Despite efficacy, cost may be a prohibitive factor. In the part of experimental materials, we found many familiar compounds, such as 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9HPLC of Formula: 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.HPLC of Formula: 106685-40-9

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

《Topical preparations for the treatment of mild-to-moderate acne vulgaris: systematic review and network meta-analysis.》 was written by Stuart, B; Maund, E; Wilcox, C; Sridharan, K; Sivaramakrishnan, G; Regas, C; Newell, D; Soulsby, I; Tang, K F; Finlay, A Y; Bucher, H C; Little, P; Layton, A M; Santer, M. Application of 106685-40-9 And the article was included in The British journal of dermatology in 2021. The article conveys some information:

BACKGROUND: Acne is very common and can have a substantial impact on wellbeing. Guidelines suggest first-line management with topical treatments, but there is little evidence regarding which treatments are most effective. OBJECTIVES: To identify the most effective and best tolerated topical treatments for acne using network meta-analysis. METHODS: CENTRAL, MEDLINE, Embase and World Health Organization Trials Registry were searched from inception to June 2020 for randomized trials that included participants with mild/moderate acne. Primary outcomes were self-reported improvement in acne, and trial withdrawal. Secondary outcomes included change in lesion counts, Investigator’s Global Assessment, change in quality of life and total number of adverse events. Network meta-analysis was undertaken using a frequentist approach. Risk of bias was assessed using the Cochrane Risk of Bias Tool and confidence in evidence was assessed using CINeMA. RESULTS: A total of 81 papers were included, reporting 40 trials with a total of 18 089 participants. Patient Global Assessment of Improvement was reported in 11 trials. Based on the pooled network estimates, compared with vehicle, benzoyl peroxide (BPO) was effective (35% vs. 26%) for improving self-reported acne. The combinations of BPO with adapalene (54% vs. 35%) or with clindamycin (49% vs. 35%) were ranked more effective than BPO alone. The withdrawal of participants from the trial was reported in 35 trials. The number of patients withdrawing owing to adverse events was low for all treatments. Rates of withdrawal were slightly higher for BPO with adapalene (2·5%) or clindamycin (2·7%) than BPO (1·6%) or adapalene alone (1·0%). Overall confidence in the evidence was low. CONCLUSIONS: Adapalene in combination with BPO may be the most effective treatment for acne but with a slightly higher incidence of withdrawal than monotherapy. Inconsistent reporting of trial results precluded firmer conclusions. In the part of experimental materials, we found many familiar compounds, such as 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9Application 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

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

《Preparation and evaluation of adapalene nanostructured lipid carriers for targeted drug delivery in acne》 was written by Ahmad Nasrollahi, Saman; Koohestani, Faezeh; Naeimifar, Atefeh; Samadi, Aniseh; Vatanara, Alireza; Firooz, Alireza. HPLC of Formula: 106685-40-9 And the article was included in Dermatologic Therapy in 2021. The article conveys some information:

Adapalene (ADA) is believed to be one of the topical treatments utilized commonly in case of acne. Nanostructured lipid carriers (NLCs) have been established as an effective carrier system with certain advantages, for instance increased solubility, drug targeting, controlled drug release, and stability of ADA. This study was conducted to obtain the formulation with a good therapeutic property. All formulations were formed by probe sonicator and its characterizations were analyzed. Finally, the therapeutic effects of 0.1% ADA-loaded nanostructured lipid carriers (NLC-ADA) were evaluated. This formulation had a great entrapment efficiency (EE) that illustrated a controlled drug release profile. A pilot clin. evaluation conducted on 15 patients (age 25.23 ± 12.24 years) with mild to moderate acne vulgaris lesions. The results demonstrated significant reduction in acne severity index and the number of inflammatory and noninflammatory lesions after 12 wk of treatment (P-value .02, .04, and .01, resp.). Subjective results were confirmed with significant improvement in size and intensity of porphyrin production in pilosebaceous follicles (P-value = .03). The study demonstrated that the formulation was safe and revealed the proper improvement rate of acne lesions after 12 wk. In the part of experimental materials, we found many familiar compounds, such as 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9HPLC of Formula: 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.HPLC of Formula: 106685-40-9

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

Niesert, Anne-Charlotte; Guertler, Anne; Reinholz, Markus published an article in 2022. The article was titled 《Short contact therapy with adapalen 0.3%/benzoyl peroxide 2.5% gel for maintenance after systemic isotretinoin treatment》, and you may find the article in Dermatologic Therapy.Quality Control of 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid The information in the text is summarized as follows:

This study report a case of a 20-yr-old woman, Fitzpatrick skin type III, who consulted our acne outpatient clinic with a distinct acne papulopustolsa, persisting for 4 years. She presented with erythematous papules, and confluent pustules, as well as numerous open and closed comedones on her face, with her cheeks predominantly affected. Clin. findings also included multiple erythematous ice pick scars and post-inflammatory hyperpigmentation. After a thorough risk-benefit anal., systemic retinoid therapy with 20 mg isotretinoin daily was initiated under strict contraception by means of a hormonal intra-uterine device (IUD). After 4 mo of treatment, the patient presented with persistent CK elevation (1728 U/L; norm <169 U/L). They decided to use adapalen 0.3%/benzoyl peroxide 2.5% gel as a SCT, recommending a daily application with subsequent wash off after 15 min. The SCT with adapalen 0.3%/benzoyl peroxide 2.5% gel continued to show significant improvement in comedones, papules, post-inflammatory hyperpigmentation and scars. In the experiment, the researchers used many compounds, for example, 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9Quality Control of 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid)

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.Quality Control of 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid

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

In 2018,Harris, Blair; Bitner, Benjamin; Thomas, Logan published 《Differin® and depilation, a word of warning.》.Journal of cosmetic dermatology published the findings.SDS of cas: 106685-40-9 The information in the text is summarized as follows:

BACKGROUND: Retinoid products are becoming increasingly popular due to their efficacy and mild side effect profile. A few cases of epidermal stripping with wax depilation have been reported, but all have been associated with oral retinoid use. AIMS: We aim to increase awareness of this adverse effect. METHODS: N/A Results: N/A Conclusion: While retinoid products are effective and have a low side effect profile, they may still cause adverse effects including the possibility of epidermal stripping with wax depilation. In the experimental materials used by the author, we found 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) may be used as a pharmaceutical reference standard for the quantification of the analyte in topical gel formulations using high-performance liquid chromatography technique.SDS of cas: 106685-40-9

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

Reference of (S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)-3-(4-sulfophenyl)propanoic acidOn June 13, 2019, Gambini, Luca; Baggio, Carlo; Udompholkul, Parima; Jossart, Jennifer; Salem, Ahmed F.; Perry, J. Jefferson P.; Pellecchia, Maurizio published an article in Journal of Medicinal Chemistry. The article was 《Covalent Inhibitors of Protein-Protein Interactions Targeting Lysine, Tyrosine, or Histidine Residues》. The article mentions the following:

We have recently reported a series of Lys-covalent agents targeting the BIR3 domain of the X-linked inhibitor of apoptosis protein (XIAP) using a benzamide-sulfonyl fluoride warhead. Using XIAP as a model system, we further investigated a variety of addnl. warheads that can be easily incorporated into binding peptides and analyzed their ability to form covalent adducts with lysine and other amino acids, including tyrosine, histidine, serine, and threonine, using biochem. and biophys. assays. Moreover, we tested aqueous, plasma stability, cell permeability, and cellular efficacy of the most effective agents. These studies identified aryl-fluoro sulfates as likely the most suitable electrophiles to effectively form covalent adducts with Lys, Tyr, and His residues, given that these agents were cell permeable and stable in aqueous buffer and in plasma. Our studies contain a number of general findings that open new possible avenues for the design of potent covalent protein-protein interaction antagonists. In the experimental materials used by the author, we found (S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)-3-(4-sulfophenyl)propanoic acid(cas: 138472-22-7Reference of (S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)-3-(4-sulfophenyl)propanoic acid)

(S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)-3-(4-sulfophenyl)propanoic acid(cas: 138472-22-7) belongs to ethers.The C-O bonds that comprise simple ethers are strong. They are unreactive toward all but the strongest bases. Although generally of low chemical reactivity, they are more reactive than alkanes. Reference of (S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)-3-(4-sulfophenyl)propanoic acid

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

The author of 《Adapalene suppressed the proliferation of melanoma cells by S-phase arrest and subsequent apoptosis via induction of DNA damage》 were Li, Hongyang; Wang, Cheng; Li, Lingjun; Bu, Wenbo; Zhang, Mengli; Wei, Jun; Tao, Lei; Qian, Kun; Ma, Pengcheng. And the article was published in European Journal of Pharmacology in 2019. Application In Synthesis of 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid The author mentioned the following in the article:

Malignant melanoma was the leading cause of mortality among the skin-associated cancer owing to its highly metastatic feature, increasing incidence and drug resistance requirement. Retinoids played important roles in the treatment of cancer via the activation of retinoid acid receptor (RAR) or retinoid X receptor (RXR). Our present study showed that the third-generation retinoid adapalene exhibited strong inhibitory effects on the proliferation of melanoma cells than other retinoids, such as all-trans-retinoic acid (ATRA), isotretinoin, acitretin and bexarotene, and adapalene exerted significant inhibitory effects on the colony formation of melanoma cells. Further study confirmed that adapalene treatment triggered dramatic S phase arrest and apoptosis, and S phase arrest was the potential mechanism of apoptosis induction. In addition, adapalene treatment dramatically regulated the expression of S phase-related protein, and increased the protein level of DNA damage marker,which were consistent with the results of the induction of the tail moment in comet assays. Meanwhile, DNA damage response was activated and the DNA repair pathway was simultaneously inhibited by adapalene treatment, which might furtherly potentiate S phase arrest and subsequent apoptosis. Taken together, these results showed that adapalene exhibited strong anti-cancer activity, and might be a candidate agent for the clin. treatment of melanoma. After reading the article, we found that the author 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)

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