ASK1-IN-1

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

ASK1-IN-1 是凋亡信号调节激酶 1 的抑制剂，该激酶 1 是凋亡和炎症细胞应激反应的关键介质，在生化检测中 IC50 为 21 nM。

ASK1-IN-1 is an inhibitor of apoptosis signal-regulating kinase 1 which is a key mediator in the apoptotic and inflammatory cellular stress response with an IC50 of 21 nM in biochemica assays.(In Vitro):ASK1-IN-1 shows good potency with cell IC50 of 138 nM. ASK1-IN-1 has superior CYP inhibition profile.(In Vivo):ASK1-IN-1 shows low clearance (rat Cl/Clu = 0.36/6.7 L h-1 kg-1) and good CNS penetration (rat K p,uu = 0.38). ASK1-IN-1 (10 mg/kg; p.o.) covers the cellular IC50/IC70/IC90 at trough in the brain for 12 hours of 50/115/435 mg/kg respectively.

ASK1-IN-1 (compound 21) has superior CYP inhibition profile and it is also inactive in a hERG assay. ASK1-IN-1 is selected for a kinase selectivity profile against a panel of 468 kinases and it is found to be moderately selective.

ASK1-IN-1 (10 mg/kg; p.o.) covers the cellular IC50/IC70/IC90 at trough in the brain for 12 hours of 50/115/435 mg/kg respectively. ASK1-IN-1 has good biochemical and cellular potency, low clearance and good brain penetration in rodents.

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Others

Other Targets

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2411382-24-4

405.41

C19H19N9O2

>98% (HPLC)

In Vitro:?DMF : 4 mg/mL (9.87 mM)

CC(C)n1c(-c2cccc(NC(c3cn(-c4nccnc4)nc3OC)=O)n2)nnc1

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(-20℃)

With Ice Pack

≥ 2 years