BMS-986251
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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- No. CAS: 2460133-35-9
- Fòrmula: C30H29F8NO5S
- Peso molecular:667.61
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Almacenamiento:
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Actividad biológica
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Actividad biológica
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RORγt 12 nM (EC50) |
IL-17 24 nM (EC50) |
RORα >10 μM (EC50) |
RORβ >10 μM (EC50) |
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Cell Line
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Type | Value | Description | References |
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| Jurkat | EC50 |
12 nM
Compound: 5; BMS-986251
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Inverse agonist activity at human Gal4-fused RORgammat expressed in human Jurkat cells assessed as inhibition of constitutive receptor activity measured after 18 hrs by steady-glo luciferase reporter gene assay
Inverse agonist activity at human Gal4-fused RORgammat expressed in human Jurkat cells assessed as inhibition of constitutive receptor activity measured after 18 hrs by steady-glo luciferase reporter gene assay
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[PMID: 32551004] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 female mice with acanthosis[1]
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Dosage:5, 15, 45 mg/kg
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Administration:Orally; twice daily until day 9
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Result:Resulted in reduced ear thickness and significantly reduces imiquimod (IMQ)-induced skin thickening.
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Animal Model:Mouse or rat[1]
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Dosage:2 mg/kg of IV and 4 mg/kg of PO (Pharmacokinetic Analysis)
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Administration:IV or PO
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2460133-35-9
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Peso molecular 667.61
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Fòrmula C30H29F8NO5S
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SMILES
O=C([C@H]1C[C@H](C)[C@H](C(N2CC[C@@]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[C@@]23[H])=O)CC1)O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BMS-986251 Related Classifications
HY-136527 Related Classifications
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