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RIPK1 inhibitor 62

Chemical Structure : RIPK1 inhibitor 62

CAS No.: 2764894-01-9

RIPK1 inhibitor 62

货号: PC-21707Not For Human Use, Lab Use Only.

RIPK1 inhibitor 62 is a potent, selective, orally bioavailable type-II kinase inhibitor of RIPK1 with IC50 of 3.5 nM (hRIPK1), 200-fold less potent against hRIPK3.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

RIPK1 inhibitor 62 is a potent, selective, orally bioavailable type-II kinase inhibitor of RIPK1 with IC50 of 3.5 nM (hRIPK1), 200-fold less potent against hRIPK3.
RIPK1 inhibitor 62 (8 nM) is able to abolish the stimulated phosphorylation and activation of RIPK1 and MLKL, and eliminates most phosphorylation of RIPK3 in FADD−/− Jurkat cells.
RIPK1 inhibitor 62 (2 mpk, p.o.) completely mitigated the acute hypothermia in mouse models of RIPK1-dependent acute or chronic inflammatory disease.
RIPK1 inhibitor 62 (15 or 30 mpk for 8 days, daily) could effectively eliminate most RA symptoms, including paw edema, erythema, and joint stiffness, without affecting the bodyweight in mice.

物理化学性质&存储条件

分子量 478.56
分子式 C27H26N8O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-5-(1-(4-(6-Amino-9H-purin-9-yl)phenyl)ethyl)-3-benzyl-2-methyl-2,5,6,7-tetrahydro-4H-pyrazolo[4,3-c]pyridin-4-one

参考文献

1. Qin Y, et al. Acta Pharm Sin B. 2024 Jan;14(1):319-334.

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