475A

Chemical Structure : 475A

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货号: PC-25179Not For Human Use, Lab Use Only.

475A is a potent, highly selective ROCK2 inhibitor with IC50 of 1.3 nM, 162-fold selective over ROCK1 (IC50=211 nM).

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25 mg		Get quote
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100 mg		Get quote

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生物&药学活性

475A is a potent, highly selective ROCK2 inhibitor with IC50 of 1.3 nM, 162-fold selective over ROCK1 (IC50=211 nM).
475A (20 or 40 mg/kg) effectively alleviates LPS-induced acute lung injury in mice.
475A (0.5-8 uM) significantly reduces the secretion of related inflammatory cytokines stimulated by LPS in macrophages.
475A (2 uM, 8 h) downregulates NLRP3 protein levels in LPS-induced THP-1 and RAW264.7 macrophages, does not affect the transcription of NLRP3.
475A increases NLRP3 ubiquitination and accelerates protein degradation via the ubiquitin-proteasome pathway.
475A induces proteasome dependent degradation of NLRP3 through the ROCK2-YAP axis and suppresses inflammation in vitro and in vivo.

物理化学性质&存储条件

分子量	469.63
分子式	C29H35N5O
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	1-(3-((((1S,3S)-3-((1H-indazol-5-yl)amino)cyclohexyl)amino)methyl)phenyl)-4-(tert-butyl)pyridin-2(1H)-one

参考文献

1. Zhan S, et al. Eur J Pharmacol. 2025 Jul 30;1004:178009.

475A

生物&药学活性

物理化学性质&存储条件

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475A

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