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HS-276
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
HS-276图片
CAS NO:2767422-72-8
包装与价格:
包装价格(元)
10mg电议
25mg电议

产品介绍
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。
Cas No.2767422-72-8
分子式C24H29N5O2
分子量419.52
溶解度DMSO : 50 mg/mL (119.18 mM; ultrasonic and warming and adjust pH to 2 with HCl and heat to 80°C)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

HS-276 is an orally active, potent and highly selectiveTAK1inhibitor, with aKiof 2.5 nM. HS-276 shows significant inhibition of TAK1, CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, withIC50values 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[1].

HS-276 reduces expression of TNF, IL-6, and IL-1β in a dose-dependent manner, with IC50values of 138, 201, and 234 nM, respectively[1].

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[1].
HS-276 (CD-1 mice, 30 mg/kg, Oral gavage, once) shows excellent bioavailability in mice with a Cmaxof 3.68 μM and %F of 98.1%[1].