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  • BMS-986143|T39129|TargetMol

BMS-986143|T39129|TargetMol

BMS-986143
10600 25mg 起订
13800 50mg 起订
17500 100mg 起订
上海 更新日期:2025-11-17

TargetMol中国(陶术生物)

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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-986143
英文名称:
BMS-986143
CAS号:
1643372-95-5
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:
T39129

Product Introduction

Bioactivity

名称BMS-986143
描述BMS-986143, an orally active, reversible BTK inhibitor with an IC50 value of 0.26 nM, is designed for autoimmune disease research. Additionally, it targets TEC, BLK, BMX, TXK, FGR, YES1, and ITK, exhibiting IC50s of 3 nM, 5 nM, 7 nM, 10 nM, 15 nM, 19 nM, and 21 nM, respectively [1].
体外活性BMS-986143 inhibits BTK with IC 50 s of 6.9±3.4 and 25±19 nM in Ramos cellular assay and the human whole blood assay, respectively [1]. BMS-986143 can effectively inhibit the end-points derived from IgG-containing immune complex low affinity activating Fcγ receptor signaling in peripheral blood mononuclear cells (PBMC) (IC 50 =2 nM) [1]. BMS-986143 inhibits the expression of CD63 on the surface of basophils in human whole blood, driven by FcεRI signaling (IC 50 of 54 nM) [1]. BMS-986143 inhibits calcium flux in Ramos B Cells, proliferation of human peripheral B Cells, CD86 surface expression in peripheral B Cells, and TNFα from human PBMC Cells with IC 50 s of 7±3, 1±0.4, 1±0.5, and 2 nM, respectively [1].
体内活性BMS-986143 shows desirable efficacy in mouse models of collagen-induced arthritis (CIA) and anticollagen antibody-induced arthritis (CAIA) [1]. BMS-986143 exhibits high oral bioavailability (mouse 100%, dog 82%) and moderate C max (mouse 4.3, dog 1.2 μM) following oral administration (mouse 6, dog 2 mg/kg) [1]. BMS-986143 exhibits long elimination half-lives (mouse 3.6, dog 7.9 h) due to moderate plasma clearance (8.6, 4.4 mL/min/kg respectively) combined with low volumes of distribution (1.8, 2.6 L/kg respectively) following intravenous administration (mouse 3.0, dog 1.0 mg/kg) [1]. Animal Model: DBA/1 male mice (8-10wk of age) bearing CIA model [1] Dosage: 15 and 45 mg/kg Administration: Oral gavage; BID Result: 15 and 45 mg/kg provided dose-dependent inhibition of observed clinical disease progression (63% and 80%, respectively), representing 17 and 19 h coverage of the mouse whole blood IC 50 (130 nM).
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-986143 | BMS986143 | BMS 986143
相关产品evobrutinib | IBT6A | Sunvozertinib | Atuzabrutinib | Edralbrutinib | Tyrosinase-IN-16 | (±)-Zanubrutinib | CP-547632 | CHMFL-EGFR-202 | Orelabrutinib | Ibrutinib | Rilzabrutinib
BMS-986143|TargetMol

公司简介

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 (13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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