Vimirogant  (Synonyms: VTP-43742)

Vimirogant (VTP-43742) is a potent, selective, and orally active RORγt inhibitor (K_i=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].

Vimirogant inhibits the secretion of IL-17A from activated hPBMCs (IC₅₀=18 nM) and human whole blood (IC₅₀=192 nM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

552.65

C₂₇H₃₅F₃N₄O₃S

1802706-04-2

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.