Vimirogant(VTP-43742)hydrochloride是一种选择性、具有口服活性的的RORγt抑制剂(Ki=3.5nM;IC50=17nM)。Vimiroganthydrochloride与RORα和RORβ比，高出>1000倍的选择性。Vimiroganthydrochloride抑制小鼠脾细胞的Th17分化和IL-17A分泌(IC50=57nM)，而不会影响Th1，Th2或Treg细胞的分化。Vimiroganthydrochloride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 (Ki=3.5 nM; IC50=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 (IC50=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 (IC50=18 nM) and human whole blood (IC50=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].
[1]. Gege C. RORγt inhibitors as potential back-ups for the phase II candidate VTP-43742 from Vitae Pharmaceuticals: patent evaluation of WO2016061160 and US20160122345. Expert Opin Ther Pat. 2017;27(1):1-8. [2]. Gerard McGeehan, et al. VTP-43742 is a potent and selective RORγt blocker that demonstrates oral efficacy in a mouse model of autoimmunity through suppression of IL-17A production (THER7P.945). J Immunol May 1, 2015, 194 (1 Supplement) 208.5-208.5.
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