1. Metabolic Enzyme/Protease
    Immunology/Inflammation
  2. ROR
    Interleukin Related
  3. BMS-986251

BMS-986251 

Cat. No.: HY-136527
Handling Instructions

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).

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BMS-986251 Chemical Structure

BMS-986251 Chemical Structure

CAS No. : 2460133-35-9

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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)[1].

IC50 & Target[1]

RORγt

12 nM (EC50)

IL-17

24 nM (EC50)

RORα

>10 μM (EC50)

RORβ

>10 μM (EC50)

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[1].

In Vivo

BMS-986251 (5-45 mg/kg; orally; twice daily until day 9) results in reduced ear thickness[1].
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)[1].
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[1].

Animal Model: C57BL/6 female mice with acanthosis[1]
Dosage: 5, 15, 45 mg/kg
Administration: Orally; twice daily until day 9
Result: Resulted in reduced ear thickness and significantly reduces imiquimod (IMQ)-induced skin thickening.
Animal Model: Mouse or rat[1]
Dosage: 2 mg/kg of IV and 4 mg/kg of PO (Pharmacokinetic Analysis)
Administration: IV or PO
Result: Had 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.
Had a Cmax of 4.8 μM and an AUC of 37 μM•h for PO in mouse.
Had a T1/2 of 11 hours, a CL of 1.3 mL/min•kg, and a Vss of 1.25 L/kg for IV in rat.
Had a Cmax of 4.7 μM and an AUC of 64 μM•h for PO in rat.
Molecular Weight

667.61

Formula

C₃₀H₂₉F₈NO₅S

CAS No.

2460133-35-9

SMILES

O=C([[email protected]]1C[[email protected]](C)[[email protected]](C(N2CC[[email protected]@]3(S(=O)(C4=CC=C(F)C=C4)=O)C5=CC=C(C(C(F)(F)F)(F)C(F)(F)F)C=C5CC[[email protected]@]23[H])=O)CC1)O

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Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

BMS-986251BMS986251BMS 986251RORInterleukin RelatedRAR-related orphan receptorILorallyacanthosisimiquimodpsoriasisPXRLXRαLXRβ?Inhibitorinhibitorinhibit

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BMS-986251
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HY-136527
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