Vimirogant

Vimirogant (VTP-43742) is a potent, selective, and orally active RORγt inhibitor (Ki=3.5 nM; IC50=17 nM) . Vimirogant exhibits >1000-fold selectivity versus the RORα and RORβ isotypes. Vimirogant inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes (IC50=57 nM) without affecting Th1, Th2, or Treg cell differentiation. Vimirogant has the potential for autoimmune disorders research[1][2].

Product Specifications

CAS Number

[1802706-04-2]

Product Name Alternative

VTP-43742

UNSPSC

12352005

Target

ROR

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/ROR_gamma_-IN-1.html

Solubility

10 mM in DMSO

Smiles

O=C(C1=CN=C([C@H](C(C)C)N(C[C@H]2CC[C@H](C(F)(F)F)CC2)C3)C3=C1)NCC4=NC=C(S(=O)(CC)=O)C=C4

Molecular Formula

C27H35F3N4O3S

Molecular Weight

552.65

References & Citations

[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.