| Bioactivity | 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]. |
| Invitro | Vimirogant inhibits the secretion of IL-17A from activated hPBMCs (IC50=18 nM) and human whole blood (IC50=192 nM)[1]. |
| In Vivo | 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]. |
| Name | Vimirogant |
| CAS | 1802706-04-2 |
| Formula | C27H35F3N4O3S |
| Molar Mass | 552.65 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |