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Chemical Structure : BMS-336
Catalog No.: PC-49023Not For Human Use, Lab Use Only.
BMS-336 is a potent, selective, orally active RORγt (RORC2) inverse agonist with EC50 of 39 nM in RORγt reporter assays.
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BMS-336 is a potent, selective, orally active RORγt (RORC2) inverse agonist with EC50 of 39 nM in RORγt reporter assays.
BMS-336 displays weak to no activity against PXR, LXRα an d LXRβ.
BMS-336 (p.o.) significantly blocked the IL-17 response in a dose-dependent manner and achieved 74% inhibition at 25 mg/kg and 98% inhibition at 100 mg/kg doses, respectively.
BMS-336 inhibited expression of RORC2-regulated genes in peripheral Th17 cells (CD4+CD25-CD127+CXCR3-CCR4+CCR6+) in a dose-dependent manner, with similar inhibitory effects on laminar propria mononuclear cells from IBD and non-IBD subjects.
BMS-336 inhibited IL-17A production and prevented inflammatory cytokine-induced destabilization in peripheral Th17-Tregs (CD4+CD25hiCD127loCXCR3-CCR4+CCR6+).
| M.Wt | 618.539 | |
| Formula | C25H26F8N2O5S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Hua Gong, et al. Bioorg Med Chem Lett. 2018 Jan 15;28(2):85-93.
2. Dominic A Boardman, et al. Eur J Immunol. 2020 Sep;50(9):1400-1411.
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