HS271

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

HS271 是一种高效、口服活性的选择性 IRAK4 抑制剂，IC50 为 7.2 μM。 HS271 表现出卓越的酶活性和细胞活性，以及优异的药代动力学特性。

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.(In Vivo):In rat models of LPS-induced TNFα production collagen-induced arthritis, HS271 (15-150 mg/kg) shows robust antiinflammatory efficacy with a t1/2 of 3.3 h and Cmax of 2107 ng/mL. The oral bioavailability of HS271 is 67.3%, 58.2%, 14.4&% and 49% in mice, rats, dogs, and monkeys, respectively.

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HS271 (15-150 mg/kg) displays robust in vivo antiinflammatory efficacy as evaluated in rat models of LPS induced TNFα production collageninduced arthritis.HS271 exhibits a t1/2 of 3.3 h and Cmax of 2107 ng/mL.HS271 is stable in liver microsome assays across other species, including rat, mouse, monkey, and human.HS271 exhibits oral bioavailability of 67.3%, 58.2%, 14.4&% and 49% in mouse, rat, dog and monkey, respectively. Animal Model:A rat model of collagen induced arthritis (CIA).Dosage:15, 50, 150 mg/kg.Administration:PO, once daily.Result:Led to a significant reduction in paw swelling as compared to vehicle control, with a minimum effective dose at 15 mg/kg QD. Notably, at 150 mg/kg QD, HS271 eliminated the paw swelling.

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Others

Other Targets

G2019S LRRK2|LRRK2

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2410393-15-4

435.44

C21H24F3N5O2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (229.65 mM)

N/A

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(-20℃)

With Ice Pack

≥ 2 years