GSK805 - ROR 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGSK805Cat. No.: HY-12776CAS No.: 1426802-50-7分式: CHClFNOS分量: 532.36作靶点: ROR作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (187.84 mM)H2O : 40% PEG30

2、0 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.70 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.70 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 GSK805种有效的RORt抑制剂。IC50 & Target IC50: 8.4 (RORt) 1.PROTOCOLAnimal Animal ad

3、ministration 1Administration 1 GSK805 are orally administered once daily at 3 doses (1, 3, and 10 mg/kg) to EAE mice from the day ofimmunization. Compared to the control, the treatment with 9a or 9g resulted in a delay and significantreduction in clinical severity of EAE in a dose-dependent manner.

4、Compared to thiazole ketone amide 2,which only showed EAE efficacy up to day 20 at 100 mg/kg twice daily dosing,32 the biaryl amides 9a and 9gare much more efficacious. This could be attributed to their good in vitro activities as well as much improvedoral exposure and CNS penetration. However, it s

5、hould be noted that although 9g had more brain exposurethan 9a, it exhibited less efficacy than 9a in EAE experiments, indicating that there might be additional factorssuch as free brain concentration affecting in vivo efficacy 1.MCE has not independently confirmed the accuracy of these methods. The

6、y are for reference only.户使本产品发表的科研献 Nat Microbiol. 2019 Mar;4(3):492-503.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Wang Y, et al. Discovery of Biaryl Amides as Potent, Orally Bioavailable, and CNS Penetrant RORt Inhibitors. ACS Med Chem Lett.2015 May 26;6(7):787-792.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 40