2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Immunology/Inflammation
  3. ROR Interleukin Related
  4. BMS-986251

BMS-986251 是一种具有口服活性的，选择性的 RORγt 反向激动剂，对 RORγt GAL4 的 EC50 为12 nM。BMS-986251 抑制 IL-17，在人全血分析中 EC50 为 24 nM。BMS-986251 在小鼠棘皮病和咪喹莫特 (Imiquimod; HY-B0180) 诱导的模型(牛皮癣的临床前模型)中显示出强大的功效。

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BMS-986251 Chemical Structure

BMS-986251 Chemical Structure

CAS No. : 2460133-35-9

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规格 价格 是否有货 数量
1 mg ￥8320
12 - 14 周
5 mg   询价  
10 mg   询价  

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BMS-986251 相关抗体

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RORγ RORα RORβ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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)[1].

IC50 & Target[1]

RORγt

12 nM (EC50)

IL-17

24 nM (EC50)

RORα

>10 μM (EC50)

RORβ

>10 μM (EC50)

体外研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

BMS-986251 相关抗体:
体内研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
分子量

667.61

Formula

C30H29F8NO5S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

BMS-986251 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BMS-9862512460133-35-9BMS986251BMS 986251RORInterleukin RelatedRAR-related orphan receptorILorallyacanthosisimiquimodpsoriasisPXRLXRαLXRβ?Inhibitorinhibitorinhibit

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目录号：
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