RIP1-IN-22

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

RIP1-IN-22 是一种高效、口服、脑穿透性 RIP1 激酶抑制剂，pKi 为 9.04。

RIP1-IN-22 is a highly potent, orally available, and brain-penetrating RIP1 kinase inhibitor with pKi of 9.04; displays excellent specificity for RIP1 kinase over 406 kinases including RIP3 kinase; strongly suppressed necroptotic cell death and phosphorylation of MLKL (pMLKL) in HT-29 cells (nectoptosis; IC50=2.0 nM, pMLKL; IC50 = 1.3 nM) as well as L929 cells (nectoptosis; IC50=15 nM, pMLKL; IC50=2.7 nM); attenuates disease progression in the mouse experimental autoimmune encephalomyelitis (EAE) model of multiple sclerosis (MS) after oral administration (10 mg/kg, bid).

RIP1 kinase inhibitor 1 (compound 22) strongly suppresses necroptotic cell death and phosphorylation of MLKL(pMLKL) in human colorectal adenocarcinoma HT-29 cells (nectoptosis, IC50=2 nM; pMLKL, IC50=1.3 nM) as well as mouse L-cells NCTC 929 (nectoptosis, IC50=15 nM; pMLKL, IC50=2.7 nM).

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Apoptosis

RIP kinase

RIP kinase

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2095515-38-9

461.906

C24H20ClN5O3

>98% (HPLC)

In Vitro:?DMSO : 200 mg/mL (432.99 mM)

N#CC1=CC=C2N(C)C([C@@H](N3CCC4=C(Cl)N(CC5=CC=CC=C5)N=C4C3=O)COC2=C1)=O

(3S)-3-(2-benzyl-3-chloro-7-oxo-2,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl)-5-methyl-4-oxo-2,3,4,5-tetrahydro-1,5-benzoxazepine-8-carbonitrile

(-20℃)

With Ice Pack

≥ 2 years