BMS-986251|T40123|TargetMol

BMS-986251
2460133-35-9

￥26600 25mg 起订

上海更新日期：2026-05-08

TargetMol中国（陶术生物）

VIP3年

联系人：邵小姐

手机：15002134094 拨打

邮箱：marketing@targetmol.cn

产品详情:

中文名称：: BMS-986251

英文名称：: BMS-986251

CAS号：: 2460133-35-9

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

产品类别：: 抑制剂

货号：: T001|T40123

Product Introduction

Bioactivity

名称	BMS-986251
描述	BMS-986251 is a potent and specific RORγt inverse agonist that exerts its action via oral administration. It shows an EC 50 of 12 nM for RORγt GAL4. In human whole blood assay, BMS-986251 effectively inhibits IL-17 with an EC 50 of 24 nM. Furthermore, BMS-986251 exhibits strong therapeutic effects in mouse acanthosis and Imiquimod-induced models, which are commonly used preclinical models for psoriasis.
体外活性	BMS-986251 is against ROR family members (RORα GAL4: EC 50 >10 μM; RORβ GAL4: EC 50 >10 μM) and against other nuclear receptors (PXR: EC 50 >5 μM; LXRα: EC 50 >7.5 μM; LXRβ: EC 50 >7.5 μM). BMS-986251 does not inhibit any of the CYP’s[1].
体内活性	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 na?ve C57BL/6 female mice (7-9 weeks)[1]. BMS-986251 (2 mg/kg of IV and 4 mg/kg of PO) has a T 1/2 of 7.7 hours, a CL of 2.7 mL/min?kg, and a V ss 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 T 1/2 of 7.7 hours, a CL of 2.7 mL/min?kg, and a V ss of 1.9 L/kg for IV in mouse. Had a C max of 4.8 μM and an AUC of 37 μM?h for PO in mouse. Had a T 1/2 of 11 hours, a CL of 1.3 mL/min?kg, and a V ss of 1.25 L/kg for IV in rat. Had a C max of 4.7 μM and an AUC of 64 μM?h for PO in rat.
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
关键字	BMS-986251 \| BMS986251 \| BMS 986251
相关产品	Rhamnose monohydrate \| Kaolin \| Ethyl palmitate \| Fluorene \| Isostearic acid \| Undecane \| Tributyrin \| Gluconate Calcium \| 1,8-Cineole \| Magnesium sulfate \| D(+)-Raffinose pentahydrate \| Hydroxypropyl Cellulose

BMS-986251;TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期	(14年)
注册资本	589.8595万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,工厂,试剂,定制,服务
主营行业	中间体,天然产物,生物化工,化学试剂,生物技术服务

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