S18-000003

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

S18-000003 是一种有效的口服生物可利用的视黄酸受体相关孤儿受体-gamma-t 抑制剂 (IC50: 29 nM)。

S18-000003 is an effective orally bioavailable retinoic acid receptor-related orphan receptor-gamma-t inhibitor (IC50: 29 nM). S18-000003 inhibits IL-17 production.

S18-000003 inhibits human and mouse RORγt-dependent transactivation, with IC50s of 0.029 and 0.34 μM respectively in cell-based GAL4 promoter reporter assays.S18-000003 (0.003-0.3 μM; 7 d) dose-dependently inhibits Th17 cell differentiation from human naive CD4+T cells, with an IC50 of 0.024 μM. S18-000003 (0.1-3 μM; 4 d) inhibits the differentiation of mouse Th17 cells from splenic naive CD4+T cells, with an IC50 of 0.20 μM.S18-000003 (0.03-1 μM; 3 d) reduces the IL-17 production in human PBMCs in a dose-dependent manner, and does not inhibit either the production of other cytokines (IL-2, IL-4, IL-10 and IFN-g) or cell proliferation.S18-000003 (0.1-3 μM; 3 d) reduces IL-17 and IL-22 production in PBMCs from psoriatic mice in a dose-dependent manner.

S18-000003 (30-100 mg/kg; p.o.) inhibits IL-17 production in the skin of IL-23-treated mice in a dose-dependent manner.S18-000003 (0.1-8%; 100mL; topically administration once daily for 14 days) ameliorates psoriasis-like lesions in TPA-induced K14.Stat3C transgenic mice, and has little impact on the thymus.S18-000003 (0.5 mg/kg; i.v.) exhibits the half-life (3.2 h), AUC (1930 ng?h/mL), CLtot (4.33 mL/min/kg) and Vdss in rats.S18-000003 (1 mg/kg; p.o.) exhibits the oral bioavailability (54.5%), Cmax (185 ng/mL), AUC (2110 ng?h/mL) and Tmax (4 h) in rats.

——

Nuclear Receptor/Transcription Factor

ROR

RORγt

——

——

2068119-11-7

518.55

C26H25F3N2O4S

>98% (HPLC)

DMSO:100 mg/mL?(192.85 mM;?Need ultrasonic)

CCS(=O)(=O)C1=CC=C(C=C1)CC(=O)NC2=CC(=C(C=C2)C(C)(C)C(=O)NC3=C(C=C(C=C3)F)F)F

——

(-20℃)

With Ice Pack

≥ 2 years