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HS271
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。
HS271图片
CAS NO:2410393-15-4
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
HS271 是一个强效的、口服有效的、选择性的 IRAK4 抑制剂,其 IC50 值为 7.2 μM。HS271 具有优越的体外酶活性和细胞活性,同时也表现出极好的药代动力学特征。
Cas No.2410393-15-4
分子式C21H24F3N5O2
分子量435.44
溶解度DMSO : 100 mg/mL (229.65 mM; Need ultrasonic)
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

HS271 is a highly potent, orally active and selective IRAK4 inhibitor, with an IC50 of 7.2 μM. HS271 exhibits superior enzymatic and cellular activities, as well as excellent pharmacokinetic properties[1].

HS271 (15-150 mg/kg) displays robust in vivo antiinflammatory efficacy as evaluated in rat models of LPS induced TNFα production collageninduced arthritis[1].HS271 exhibits a t1/2 of 3.3 h and Cmax of 2107 ng/mL[1].HS271 is stable in liver microsome assays across other species, including rat, mouse, monkey, and human[1].HS271 exhibits oral bioavailability of 67.3%, 58.2%, 14.4&% and 49% in mouse, rat, dog and monkey, respectively[1].

[1]. Wenqiang Zhai, et al. Discovery and optimization of a potent and selective indazolamine series of IRAK4 inhibitors. Bioorg Med Chem Lett. 2020 Nov 24;31:127686.