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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]. | [in vivo]
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]. | [IC 50]
RORγt: 3.5 nM (Ki); RORγt: 17 nM (IC50) | [References]
[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. DOI:10.1080/13543776.2017.1262350
[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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