Chemical Structure : 475A
CAS No.:
3000542-01-5
475A
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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469.63
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Formula
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C29H35N5O
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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1-(3-((((1S,3S)-3-((1H-indazol-5-yl)amino)cyclohexyl)amino)methyl)phenyl)-4-(tert-butyl)pyridin-2(1H)-one
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References
1. Zhan S, et al. Eur J Pharmacol. 2025 Jul 30;1004:178009.
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