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编 号：F618139
分子式：C30H29F8NO5S
分子量：667.61
分子式：C30H29F8NO5S
分子量：667.61
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CAS No: 2460133-35-9
产品详情
生物活性：
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).
体内研究：
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 na?ve 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. Animal Model:C57BL/6 female mice with acanthosis
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
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.
体外研究：
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.
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).
体内研究：
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 na?ve 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. Animal Model:C57BL/6 female mice with acanthosis
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
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.
体外研究：
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.
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