RORγt inverse agonist 13

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

RORγt 反向激动剂 13 (Compound 3i) 是一种有效的、口服活性的、选择性的 RORγt 反向激动剂 (IC50=63.8 nM)，具有改善的化合物样特性。

RORγt inverse agonist 13 (Compound 3i) is a potent, orally active and selective RORγt inverse agonist (IC50=63.8 nM), with improved drug-like properties.(In Vitro):RORγt inverse agonist 13 (Compound 3i) shows an inhibition of 76% at 0.3?μM in Th17 cell differentiation assay.(In Vivo):RORγt inverse agonist 13 (Compound 3i, 25 mg/kg, Orally, twice daily) demonstrats excellent in vivo PK profile in mice and good in vivo efficacy in an IMQ-induced psoriasis mice model.

RORγt inverse agonist 13 (Compound 3i) exhibits activity with an inhibition of 76% at 0.3?μM in Th17 cell differentiation assay.

RORγt inverse agonist 13 (Compound 3i, 25 mg/kg, Orally, twice daily) demonstrats excellent in vivo PK profile in mice and good in vivo efficacy in an IMQ-induced psoriasis mice model. Animal Model:Imiquimod (IMQ)-induced psoriasis mice model.Dosage:25 mg/kg.Administration:Orally, twice daily.Result:Brought in a significant reduction in clinical severity of psoriasis as measured through the ear erythema, back skin erythema and scaliness scales.Animal Model:Male CD-1 Mice.Dosage:1 mg/kg (i.v.) and 5 mg/kg (p.o.)(Pharmacokinetic Analysis).Administration:IV or PO, single dose.Result:Cmax: 609.67 ng/mL (PO), 1550 ng/mL (IV).

——

Nuclear Receptor/Transcription Factor

ROR

Cholinergic| Histamine relase

——

——

2170477-75-3

513.29

C23H17Cl2F3N2O4

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (194.82 mM)

OC(Cc1ccc(CNC(Nc2cc(Cl)c(-c(cccc3)c3OC(F)(F)F)c(Cl)c2)=O)cc1)=O

——

(-20℃)

With Ice Pack

≥ 2 years