Description
BMS-986251 is an orally active and selective RORγt inverse agonist with an EC50 of 12 nM for RORγt GAL4. BMS-986251 inhibits IL-17 with an EC50 of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced (HY-B0180) models (preclinical models of psoriasis).
Product information
CAS Number: 2460133-35-9
Molecular Weight: 667.61
Formula: C30H29F8NO5S
Chemical Name: (1R,3S,4R)-4-[(3aR,9bR)-9b-(4-fluorobenzenesulfonyl)-7-(1,1,1,2,3,3,3-heptafluoropropan-2-yl)-1H,2H,3H,3aH,4H,5H,9bH-benzo[e]indole-3-carbonyl]-3-methylcyclohexane-1-carboxylic acid
Smiles: C[C@H]1C[C@@H](CC[C@H]1C(=O)N1CC[C@@]2([C@H]1CCC1=CC(=CC=C21)C(F)(C(F)(F)F)C(F)(F)F)S(=O)(=O)C1C=CC(F)=CC=1)C(O)=O
InChiKey: JQORWGARJVSRBA-QOTTZFGFSA-N
InChi: InChI=1S/C30H29F8NO5S/c1-16-14-18(26(41)42)2-9-22(16)25(40)39-13-12-27(45(43,44)21-7-5-20(31)6-8-21)23-10-4-19(15-17(23)3-11-24(27)39)28(32,29(33,34)35)30(36,37)38/h4-8,10,15-16,18,22,24H,2-3,9,11-14H2,1H3,(H,41,42)/t16-,18+,22+,24+,27+/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
BMS-986251 is against ROR family members (RORα GAL4: EC50>10 μM; RORβ GAL4: EC50>10 μM) and against other nuclear receptors (PXR: EC50>5 μM; LXRα: EC50>7.5 μM; LXRβ: EC50>7.5 μM). BMS-986251 does not inhibit any of the CYP’s.
In Vivo:
BMS-986251 (5-45 mg/kg; orally; twice daily until day 9) results in reduced ear thickness. BMS-986251 (0.13, 0.79, 4.76 mg/kg; orally; once a day) displays a dose-dependent reduction of the IL-17F produced in naïve C57BL/6 female mice (7-9 weeks). BMS-986251 (2 mg/kg of IV and 4 mg/kg of PO) has a T1/2 of 7.7 hours, a CL of 2.7 mL/min•kg, and a Vss of 1.9 L/kg for IV in mouse.
Products are for research use only. Not for human use.
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