Tag: 400-500

Application of 106685-40-9In 2021 ,《Discovery of small-molecule inhibitors of SARS-CoV-2 proteins using a computational and experimental pipeline》 was published in Frontiers in Molecular Biosciences. The article was written by Lau, Edmond Y.; Negrete, Oscar A.; Bennett, W. F. Drew; Bennion, Brian J.; Borucki, Monica; Bourguet, Feliza; Epstein, Aidan; Franco, Magdalena; Harmon, Brooke; He, Stewart; Jones, Derek; Kim, Hyojin; Kirshner, Daniel; Lao, Victoria; Lo, Jacky; McLoughlin, Kevin; Mosesso, Richard; Murugesh, Deepa K.; Saada, Edwin A.; Segelke, Brent; Stefan, Maxwell A.; Stevenson, Garrett A.; Torres, Marisa W.; Weilhammer, Dina R.; Wong, Sergio; Yang, Yue; Zemla, Adam; Zhang, Xiaohua; Zhu, Fangqiang; Allen, Jonathan E.; Lightstone, Felice C.. The article contains the following contents:

A rapid response is necessary to contain emergent biol. outbreaks before they can become pandemics. The novel coronavirus (SARS-CoV-2) that causes COVID-19 was first reported in Dec. of 2019 in Wuhan, China and reached most corners of the globe in less than two months. In just over a year since the initial infections, COVID-19 infected almost 100 million people worldwide. Although similar to SARS-CoV and MERS-CoV, SARS-CoV-2 has resisted treatments that are effective against other coronaviruses. Crystal structures of two SARS-CoV-2 proteins, spike protein and main protease, have been reported and can serve as targets for studies in neutralizing this threat. We have employed mol. docking, mol. dynamics simulations, and machine learning to identify from a library of 26 million mols. possible candidate compounds that may attenuate or neutralize the effects of this virus. The viability of selected candidate compounds against SARS-CoV-2 was determined exptl. by biolayer interferometry and FRET-based activity protein assays along with virus-based assays. In the pseudovirus assay, imatinib and lapatinib had IC50 values below 10μM, while candesartan cilexetil had an IC50 value of approx. 67μM against Mpro in a FRETbased activity assay. Comparatively, candesartan cilexetil had the highest selectivity index of all compounds tested as its half-maximal cytotoxicity concentration 50 (CC50) value was the only one greater than the limit of the assay (>100μM). In the experiment, the researchers used many compounds, for example, 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) 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 of 106685-40-9

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Application In Synthesis of 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acidIn 2022 ,《Drug repurposing of adapalene for melanoma treatment》 appeared in Pharmaceutical Patent Analyst. The author of the article were Anaya-Ruiz, Maricruz; Perez-Santos, Martin. The article conveys some information:

A review. Cancer drug repurposing is an attractive approach that leads to savings in time and investment. Adapalene, the first medical application of which was for the treatment of acne, has been described as a repurposing drug for the treatment of various types of cancer. Patent application CN111329851 describes the use of adapalene for the treatment of melanoma, by assays carried out on melanoma cell lines. Adapalene demonstrated antiproliferative activity in melanoma cell lines via S-phase arrest-dependent apoptosis mediated by DNA damage through an increase in the expression of p-ATM and p-chk2 and a decrease in the expression of p-BRCA1 and Rad51. Even though no evidence on efficacy and efficiency is shown in preclin. and clin. studies, CN111329851 patent shows that adapalene may be a repurposing drug for the treatment of melanoma. In the experimental materials used by the author, we found 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

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Recommanded Product: 324017-21-2On November 13, 2017 ,《Library design-facilitated high-throughput sequencing of synthetic peptide libraries》 appeared in ACS Combinatorial Science. The author of the article were Vinogradov, Alexander A.; Gates, Zachary P.; Zhang, Chi; Quartararo, Anthony J.; Halloran, Kathryn H.; Pentelute, Bradley L.. The article conveys some information:

A methodol. to achieve high-throughput de novo sequencing of synthetic peptide mixtures is reported. The approach leverages shotgun nanoliquid chromatog. coupled with tandem mass spectrometry-based de novo sequencing of library mixtures (up to 2000 peptides) as well as automated data anal. protocols to filter away incorrect assignments, noise, and synthetic side-products. For increasing the confidence in the sequencing results, mass spectrometry-friendly library designs were developed that enabled unambiguous decoding of up to 600 peptide sequences per h while maintaining greater than 85% sequence identification rates in most cases. The reliability of the reported decoding strategy was addnl. confirmed by matching fragmentation spectra for select authentic peptides identified from library sequencing samples. The methods reported here are directly applicable to screening techniques that yield mixtures of active compounds, including particle sorting of one-bead one-compound libraries and affinity enrichment of synthetic library mixtures performed in solution In the part of experimental materials, we found many familiar compounds, such as Fmoc-D-Phe(4-NH2)-OH(cas: 324017-21-2Recommanded Product: 324017-21-2)

Fmoc-D-Phe(4-NH2)-OH(cas: 324017-21-2) belongs to ethers.Recommanded Product: 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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《Acne and rosacea in skin of colour.》 was written by Maruthappu, T; Taylor, M. Recommanded Product: 106685-40-9 And the article was included in Clinical and experimental dermatology in 2021. The article conveys some information:

Acne and rosacea are common inflammatory skin conditions present in numerous racial and ethnic groups. There are distinct differences in clinical presentation, exacerbating factors, potential triggers and consequences of both conditions in individuals with skin of colour (SOC), classified as Fitzpatrick skin types III-VI. For example, acne can be complicated by the development of postinflammatory hyperpigmentation and keloid scarring in SOC, and this can influence treatment choice. Although rosacea is reported less frequently in SOC, this may be the result of delayed diagnosis or late presentation due to the difficulty in discerning the classic features of erythema in darker skin tones. In such cases, additional clues in the medical history and clinical examination may assist in making the diagnosis. This review aims to summarize nuances in both the diagnosis and management of these two common skin conditions in patients with SOC to support clinicians in providing an individualized treatment approach. In the experiment, the researchers used many compounds, for example, 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9Recommanded Product: 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.Recommanded Product: 106685-40-9

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Salimi, Anayatollah; Emam, Monasadat; Mohammad Soleymani, Saeed published their research in Journal of cosmetic dermatology in 2021. The article was titled 《Increase adapalene delivery using chemical and herbal enhancers.》.Application of 106685-40-9 The article contains the following contents:

BACKGROUND: Acne is one of the skin diseases that include abnormalities in the production of sebum, changes in the microbial flora, abnormal keratinization, and inflammation. Adapalene is a good choice in the treatment of acne with fewer side effects and high effectiveness. However, the absorption of adapalene through human skin is low. We investigated the effect of several enhancers on the skin absorption of adapalene. METHODS: For the preparation of a topical formulation, this drug needs proper skin absorption. Therefore, to increase the effect of chemical absorption of the Adapalene skin permeability, it should first be put on the skin in a touch of some absorption like Eucalyptus, Urea, Clove oil, propylene glycol, and oleic acid for 1 and 2 hours and was then examined for the passing of the drug on the treated skin and for the effect of absorptions by calculating of the permeability parameters using DSC and FT-IR techniques. RESULT AND CONCLUSION: The results show that the enhancers used increased the permeability of the drug adapalene to water. Several mechanisms including lipid liquefaction, degradation of the fat structure, as well as irreversible denaturation of intracellular creatine caused by Eucalyptus, urea clove oil, PG, and oleic acid are the main mechanisms of drug penetration. Based on the results, it was found that among the enhancers studied, eucalyptus and urea had the highest and the lowest absorption effect in 2- and 1-hour pre-contact, respectively. In the experimental materials used by the author, we found 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) 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 of 106685-40-9

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

In 2019,Asian Journal of Pharmaceutics included an article by Shrivastava, Birendra; Sunil, Mekala; Kishore, V. Sai. COA of Formula: C28H28O3. The article was titled 《Topical combination delivery of benzoyl peroxide and adapalene niosomal gel for acne treatment》. The information in the text is summarized as follows:

Aim and Objective: Adapalene (ADP) is very effective in 0.01% strength, but it causes skin erythema in the applied area. ADP and benzoyl peroxide (BPO) are the most commonly used drugs in treatment of acne. Materials and Methods: The non-ionic surfactants like SPANs are obtained from synthetic sources, and hence the quality is maintained same all the time. The ADP was incorporated into niosomes using SPAN 60 and cholesterol was used as a stabilizer. Various ratios of SPAN 60, cholesterol, Stearic acid, BPO, and ADP were tried and optimized. The present study investigates the effect of niosomal coadministration of BPO and ADP in term of in vitro skin retention study and in vivo antiacne effects. These vesicular carriers, because of their improved percutaneous delivery and better skin retention, have proved to be very useful in enhancing therapeutic index of drugs used for tropical diseases. The niosomal dispersion was incorporated into Carbopol gel. The gel was kept for 3 mo accelerated stability studies. Results and Discussion: The niosomal dispersion was evaluated for various parameters such as vesicle size, shape, and morphol. by transmission electron microscopy. The drug release pattern from gel was evaluated on the basis of in vitro studies and skin irritation studies on rabbit skin. Conclusion: The in vitro study shows sustained release gel effects whereas the in vivo study shows no signs of irritation on the applied skin area. The results came from multiple reactions, including the reaction of 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9COA of Formula: C28H28O3)

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.COA of Formula: C28H28O3

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

In 2022,Patricio, Rui P. S.; Videira, Paula A.; Pereira, Florbela published an article in Bioorganic & Medicinal Chemistry. The title of the article was 《A computer-aided drug design approach to discover tumour suppressor p53 protein activators for colorectal cancer therapy》.Synthetic Route of C28H28O3 The author mentioned the following in the article:

Colorectal cancer (CRC) is the third most detected cancer and the second foremost cause of cancer deaths in the world. Intervention targeting p53 provides potential therapeutic strategies, but thus far no p53-based therapy has been successfully translated into clin. cancer treatment. Here we developed a Quant. Structure-Activity Relationships (QSAR) classification models using empirical mol. descriptors and fingerprints to predict the activity against the p53 protein, using the potency value with the active or inactive label, were developed. These models were built using in total 10,505 mols. that were extracted from the ChEMBL, ZINC and Reaxys databases, and recent literature. Three machine learning (ML) techniques e.g., Random Forest, Support Vector Machine, Convolutional Neural Network were explored to build models for p53 inhibitor prediction. The performances of the models were successfully evaluated by internal and external validation. Moreover, based on the best in silico p53 model, a virtual screening campaign was carried out using 1443 FDA-approved drugs that were extracted from the ZINC database. A list of virtual screening hits was assented on base of some limits established in this approach, such as: (1) probability of being active against p53; (2) applicability domain; (3) prediction of the affinity between the p53, and ligands, through mol. docking. The most promising according to the limits established above was dihydroergocristine. This compound revealed cytotoxic activity against a p53-expressing CRC cell line with an IC50 of 56.8μM. This study demonstrated that the computer-aided drug design approach can be used to identify previously unknown mols. for targeting p53 protein with anti-cancer activity and thus pave the way for the study of a therapeutic solution for CRC. The experimental part of the paper was very detailed, including the reaction process of 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

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

《Synthesis and antiageing properties of antioxidant pseudopeptides designed based on the bioisostere principle》 was published in Archiv der Pharmazie (Weinheim, Germany) in 2019. These research results belong to Li, Yanbing; Zhang, Chao; Wang, Huailing; Zhou, Fan; Liu, Jie; Tang, Yinying; Jiang, Zhenlei; Liu, Zhijun; Chen, Heru. COA of Formula: C24H22N2O4 The article mentions the following:

Nineteen antioxidant pseudopeptides were designed and synthesized. They were confirmed as mild antioxidants, in which L1-11 was the most active antioxidant with a cellular antioxidant activity (CAA) value of 5.65 ± 0.64 μmol QE/g, and L1-12 was the second most active one (5.58 ± 0.66 μmol QE/g). The existence of nonnatural amino acids in L1-12 increased its stability. Pretreatment with L1-12 dose-dependently extended the lifespan of Caenorhabditis elegans. L1-12 improved resistance against UVB irradiation, oxidative stress induced by paraquat, and thermal shock. It decreased the reactive oxygen species level and upregulated the superoxide dismutase activity inside C. elegans. This pseudopeptide sensitively enhanced the expressions of the Cat-1 and Nhr-8 genes to reduce oxidative damage, leading to an extension of the lifespan. All the evidence support that L1-12 may probably be a potential antiageing agent. 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.The C-O bonds that comprise simple ethers are strong. COA of Formula: C24H22N2O4 They are unreactive toward all but the strongest bases. Although generally of low chemical reactivity, they are more reactive than alkanes.

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

In 2019,Dermatology (Basel, Switzerland) included an article by Donnarumma, Marianna; Fattore, Davide; Greco, Vincenzo; Ferrillo, Maria; Vastarella, Maria; Chiodini, Paolo; Fabbrocini, Gabriella. Formula: C28H28O3. The article was titled 《How to Increase Adherence and Compliance in Acne Treatment A Combined Strategy of SMS and Visual Instruction Leaflet》. The information in the text is summarized as follows:

Acne is a common skin disease with important psychosocial impact. Often inadequate compliance affects the efficacy of the therapy. Because of emerging use of mobile and electronic health technol., the recent literature evaluated the helpfulness of the tools in medication adherence. The first goal of our study was to evaluate the adherence to therapy with topical adapalene 0.3%/benzoyl peroxide (A-BPO) 2.5% in different groups of patients who received explicative information supported by different strategies. The second goal was to evaluate the patient’s quality of life and skin parameters. We enrolled 126 subjects with mild to severe acne vulgaris. They were randomized into 3 groups of 42 patients each and applied daily topical A-BPO (0.3%, 2.5%) for 12 wk. After 12 wk of therapy, we observed a reduction in IGA in all groups confirming the clin. efficacy of the product. We observed that adherence days correlated pos. with the improvement of the single parameters. Moreover, we observed that SMS and leaflet groups had a greater improvement in quality of life evaluated by CADI and PDRDS scores. Conclusions: According to our data, this exptl. setup based on text message service and leaflet service is inexpensive and easy to use. Physicians could consider using these items in their practice to enhance patient adherence and satisfaction as well as treatment outcome.6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9Formula: C28H28O3) 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.Formula: C28H28O3

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Ether – Wikipedia,
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《Safe Use of Adapalene 0.1 % Gel in a non-Prescription Environment.》 was written by Weiss, Jonathan; Mallavalli, Sreenadh; Meckfessel, Matthew; Griffin, Sean; Wagner, Nathalie. Category: ethers-buliding-blocks And the article was included in Journal of drugs in dermatology : JDD in 2021. The article conveys some information:

BACKGROUND: Topical retinoids are the mainstay of acne therapy and, until 2016, were only available by prescription. The margin of safety (MOS) of adapalene for potential teratogenic effects, and its use in pregnancy were investigated as part of the OTC switch. OBJECTIVE: To determine MOS using a maximal usage trial (MUsT) and animal embryo-fetal development studies. To conduct a thorough review of safety data with respect to use of Adapalene 0.1% Gel during pregnancy. METHODS: The MUsT was multicenter, open-label pharmacokinetic study which enrolled adolescents and adult subjects with mainly severe acne vulgaris. The no observable adverse event level (NOAEL) for adapalene teratogenicity was established in rat and rabbit embryo-fetal development studies. An exhaustive review of pregnancy data from multiple safety databases was conducted. RESULTS: The calculated MOS for teratogenicity was 70 for Adapalene 0.1% Gel. For the pregnancy safety review, no pregnancy malformations were attributable to topical adapalene use. LIMITATIONS: Animal studies do not always predict effects in human development. Additionally, safety data is voluntarily reported and intrinsically incomplete. CONCLUSION: Adapalene has a large and reassuring MOS making it suitable for OTC use. No teratogenic risk was identified in a MUsT and Pregnancy Safety Review. Adapalene 0.1% Gel is a safe and effective medication for the treatment of acne in a non-prescription environment. Based on available evidence, use of adapalene during pregnancy does not pose harm to the fetus. J Drugs Dermatol. 2021;20(12):1330-1335. doi:10.36849/JDD.6527. In the part of experimental materials, we found many familiar compounds, such as 6-(3-(Adamantan-1-yl)-4-methoxyphenyl)-2-naphthoic acid(cas: 106685-40-9Category: 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

Referemce:
Ether – Wikipedia,
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