HS-276
目录号: PL04192 纯度: ≥98%
CAS No. :2767422-72-8
商品编号 规格 价格 会员价 是否有货 数量
PL04192-5mg 5mg 询价 询价
PL04192-10mg 10mg 询价 询价
PL04192-25mg 25mg 询价 询价
PL04192-50mg 50mg 询价 询价
PL04192-100mg 100mg 询价 询价
PL04192-10mM*1mLinDMSO 10mM*1mLinDMSO 询价 询价
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中文名称
HS-276
英文名称
HS-276
英文别名
HS-276
Cas No.
2767422-72-8
分子式
C24H29N5O2
分子量
419.52
包装储存
Powder -20°C 3 years;In solvent -80°C 6 months
产品详情
HS-276 是一种口服有效且高选择性的 TAK1 抑制剂,Ki 值为 2.5 nM。HS-276 对 TAK1、CLK2、GCK、ULK2、MAP4K5、IRAK1、NUAK、CSNK1G2、CAMKKβ-1 和 MLK1 具有显著抑制作用,IC50 值分别为 8.25、29、33、63、125、264、270、810、1280 和 5585 nM。HS-276 可用于类风湿关节炎 (RA) 研究。
生物活性
HS-276 is an orally active, potent and highly selective TAK1 inhibitor, with a K i of 2.5 nM. HS-276 shows significant inhibition of TAK1, CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with IC 50 values of 8.25, 29, 33, 63, 125, 264, 270, 810, 1280, and 5585 nM, respectively. HS-276 can be used for rheumatoid arthritis (RA) research.
性状
Solid
IC50 & Target[1][2]
IRAK1 264 nM (IC50) IRAK4 2500 nM (IC
体外研究(In Vitro)
HS-276 reduces expression of TNF, IL-6, and IL-1β in a dose-dependent manner, with IC50 values of 138, 201, and 234 nM, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
HS-276 (CIA mouse model of inflammatory arthritis, 50 mg/kg, IP, daily for 6 days) reduces inflammation, pannus, cartilage damage (CD), bone resorption (BR), and periosteal bone formation (PBF) histological manifestations.
HS-276 (CD-1 mice, 30 mg/kg, Oral gavage, once) shows excellent bioavailability in mice with a C max of 3.68 μM and %F of 98.1%. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[1]. Scarneo S, et al. Development and Efficacy of an Orally Bioavailable Selective TAK1 Inhibitor for the Treatment of Inflammatory Arthritis. ACS Chem Biol. 2022 Mar 18;17(3):536-544.
溶解度数据
In Vitro: DMSO : 50 mg/mL (119.18 mM; ultrasonic and warming and adjust pH to 2 with HCl and heat to 80°C)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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