Camostat Mesilate

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抑制剂描述：

产品名称：Camostat Mesilate

产品别名：见爱必信官网

英文别名：Camostat Mesilate

靶点：Sodium Channel

CAS：59721-29-8

纯度：>98%

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

Camostat is a trypsin-like protease inhibitor, inhibits airway epithelial sodium channel (ENaC) function with IC50 of 50 nM, less potent to trpsin, prostasin and matriptase.

溶解性：DMSO ：49.5 mg/mL (100 mM)；
Water ：49.5 mg/mL (100 mM)

体外研究：

Camostat (30 μM) prolongs attenuation of ENaC function in human airway epithelial cell models that is reversible upon the addition of excess trypsin. Camostat mesilate (500 mM) inhibits generation of TGF-beta by suppressing plasmin activity and reduces the activity of TGF-beta, which blocks in vitro activation of HSCs. Camostat mesilate (20 mM) combined with insulin results a significant hypoglycemic effect following large intestinal administration. Camostat mesilate (20 mM) is effective in reducing insulin degradation in both small and large intestinal homogenates of rats. Camostat mesilate (2 mM) inhibits MCP-1 and TNF- production in activated rat monocytes. Camostat mesilate (2 mM) inhibits proliferation and MCP-1 production of cultured rat PSCs.

体内研究：Camostat (100 μg/kg i.t.) induces a potent and prolonged attenuation of ENaC activity in the guinea pig trachea. Camostat mesilate (1-2 mg/g of diet) markedly attenuats an increase in hepatic plasmin and TGF-beta levels, HSC activation, and hepatic fibrosis without apparent systemic or local side effects in porcine serum–treated rats. Camostat mesilate (1 mg/g) prevents pancreatic atrophy and improves pancreatic exocrine function of rat chronic pancreatitis induced by DBTC. Camostat mesilate (1 mg/g) inhibits chronic inflammation and pancreatic fibrosis induced by DBTC. Camostat mesilate (1 mg/g) inhibits the development of pancreatic fibrosis and PSCs activation in the pancreas induced by DBTC. Camostat mesilate (1 mg/g) suppresses monocytes infiltration and inhibits MCP-1 expression both in serum and in pancreatic tissue. Camostat mesilate (100 mg/kg) significantly increases the body weight and pancreatic wet weight, and it significantly inhibits inflammatory changes and fibrosis of the pancreas through the suppression of gene expressions of PAP, p8, and cytokines in rat chronic pancreatitis.

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