HS271

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。

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库存: 现货

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包装

价格

促销价

数量
5mg

￥3775.00

3020.00

- +
10mg

￥6262.00

5010.00

- +
25mg

￥11875.00

9500.00

- +
50mg

￥18162.00

14530.00

- +
100mg

￥26712.00

21370.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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货号: ajcx33704
CAS: 2410393-15-4
别名:
分子式: C21H24F3N5O2
分子量: 435.44
纯度: >98%
溶解度: DMSO : 100 mg/mL (229.65 mM; Need ultrasonic)
储存: Store at -20°C
库存: 现货

Background

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.