Vimirogant (VTP-43742) hydrochloride 是一种选择性、具有口服活性的的RORγt抑制剂 (Ki=3.5 nM;IC50=17 nM)。Vimirogant hydrochloride 与 RORα 和 RORβ 比，高出 >1000 倍的选择性。Vimirogant hydrochloride 抑制小鼠脾细胞的 Th17 分化和 IL-17A 分泌 (IC50=57 nM)，而不会影响 Th1，Th2 或 Treg 细胞的分化。Vimirogant hydrochloride可用于研究自身免疫性疾病研究。

Vimirogant (VTP-43742) hydrochloride is a potent, selective, and orally active RORγt inhibitor ( K i =3.5 nM; IC 50 =17 nM). Vimirogant hydrochloride exhibits >1000-fold selectivity versus the RORα and RORβ isotypes. Vimirogant hydrochloride inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes (IC 50 =57 nM) without affecting Th1, Th2, or Treg cell differentiation. Vimirogant hydrochloride has the potential for autoimmune disorders research [1] [2].

Vimirogant hydrochloride inhibits the secretion of IL-17A from activated hPBMCs (IC 50 =18 nM) and human whole blood (IC 50 =192 nM) [1].

In the MOG35-55/CFA immunized mouse EAE model, Vimirogant hydrochloride (p.o.) significantly suppresses clinical symptoms, demyelination and mRNA expression of multiple inflammatory markers in the spinal cord [1].

C27H36ClF3N4O3S

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years