ROR gamma-t-IN-1

Modify Date: 2024-01-12 06:03:16

Use of ROR gamma-t-IN-1

GSK805 is a potent, orally bioavailable RORγγ Inhibitor with pIC50 of 8.4 and >8.2 for RORγ FRET assay and Th17 assay.

Name	N-[2,6-Dichloro-2'-(trifluoromethoxy)-4-biphenylyl]-2-[4-(ethylsulfonyl)phenyl]acetamide
Synonym	More Synonyms

Description	GSK805 is a potent, orally bioavailable RORγγ Inhibitor with pIC50 of 8.4 and >8.2 for RORγ FRET assay and Th17 assay.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> ROR Research Areas >> Inflammation/Immunology
Target	IC50: 8.4 (RORγt)[1].
Animal Admin	Animal administration[1] GSK805 are orally administered once daily at 3 doses (1, 3, and 10 mg/kg) to EAE mice from the day of immunization. Compared to the control, the treatment with 9a or 9g resulted in a delay and significant reduction in clinical severity of EAE in a dose-dependent manner. 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 9g are much more efficacious. This could be attributed to their good in vitro activities as well as much improved oral exposure and CNS penetration. However, it should be noted that although 9g had more brain exposure than 9a, it exhibited less efficacy than 9a in EAE experiments, indicating that there might be additional factors such as "free" brain concentration affecting in vivo efficacy[1].
References	[1]. Wang Y, et al. Discovery of Biaryl Amides as Potent, Orally Bioavailable, and CNS Penetrant RORγt Inhibitors. ACS Med Chem Lett. 2015 May 26;6(7):787-792.

MFCD28902182

Benzeneacetamide, N-[2,6-dichloro-2'-(trifluoromethoxy)[1,1'-biphenyl]-4-yl]-4-(ethylsulfonyl)-

N-[2,6-Dichloro-2'-(trifluoromethoxy)-4-biphenylyl]-2-[4-(ethylsulfonyl)phenyl]acetamide

ROR gamma-t-IN-1

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Price: ￥4099/10 mM * 1 mL in DMSO

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