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GNS-3595

Chemical Structure : GNS-3595

CAS No.:

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GNS-3595 (GNS3595)

Catalog No.: PC-22511Not For Human Use, Lab Use Only.

GNS-3595 is a potent and selective ROCK2 inhibitor with IC50 of 5.7 nM, 80-fold selectivity over ROCK1 at 1mM ATP.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

GNS-3595 is a potent and selective ROCK2 inhibitor with IC50 of 5.7 nM, 80-fold selectivity over ROCK1 at 1mM ATP.
GNS-3595 inhibits pMLC activity in various cellines, and significantly down-regulates pro-fibrotic proteins such as co lagen, fibronectin, αSMA and CTGF in IPF cells, and suppresss TGF-β-induced FMT in NHLF cells.
GNS-3595 exhibits excellent oral bioavailability and drug-like properties.
GNS-3595 suppresses pulmonary lung fibrosis in a bleomycin-induced in vivo mouse model, stabilizes body weight loss and prevents fibrosis-induced lung weight gain.
GNS-3595 at oral dose of 0.1, 0.3 or 1 mg/kg once daily, showed a significant reduction in Ashcroft scores, colagen, and αSMA, in a dose-dependent manner.

Physicochemical Properties

M.Wt
Formula
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

References

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