Camostat Mesilate

製品コードS2874 バッチS287401

化学情報

	Synonyms	FOY-305, FOY-S980	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₀H₂₂N₄O₅.CH₄O₃S
	分子量	494.52	CAS No.	59721-29-8
Solubility (25°C)*	体外	DMSO	99 mg/mL (200.19 mM)
		Water	10 mg/mL (20.22 mM)
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Camostat (FOY-305, FOY-S980) 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.
in vitro	Camostat (30 μM) prolongs attenuation of ENaC function in human airway epithelial cell models that is reversible upon the addition of excess trypsin. ^[1] 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. ^[2] 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. ^[3] 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. ^[4]
in vivo	Camostat (100 μg/kg i.t.) induces a potent and prolonged attenuation of ENaC activity in the guinea pig trachea. ^[1] 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. ^[2] 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. ^[4] 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. ^[5]

プロトコル(参考用のみ)

キナーゼアッセイ	Binding assay
キナーゼアッセイ	Enzymes are diluted into the appropriate activity buffer (prostasin, matriptase, and trypsin: 15 mM HEPES, pH 7.4, 25 mM NaCl, and 0.5% CHAPS; furin: 15 mM HEPES, pH 7.6, 25 mM NaCl, 1 mM CaCl₂, 1 mM β-mercaptoethanol, and 0.5% CHAPS; HNE: 15 mM HEPES, pH 7.6, 150 mM NaCl, and 0.75% CHAPS), added to compound solutions, and incubated at room temperature for 20 min. Fluorogenic substrates are mixed with activity buffer and added to the enzyme/compound solution after the 20-min incubation. Fluorescence emission is quantified on a Gemini plate reader at 37°C. Excitation wavelength is 380 nm, emission wavelength is 450 nm, and cut-off is 435 nm. Ki values are determined through analysis of progression curves using BioKin PlateKi.
動物実験	動物モデル	male Wistar rats
	投薬量	2 mg/g
	投与方法	Diet

参考

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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Glycopeptide Antibiotic Teicoplanin Inhibits Cell Entry of SARS-CoV-2 by Suppressing the Proteolytic Activity of Cathepsin L [ Front Microbiol, 2022, 13:884034]	PubMed: 35572668
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TMPRSS2 and TMPRSS4 Promote SARS-CoV-2 Infection of Human Small Intestinal Enterocytes [ Sci Immunol, 2020, 13;5(47):eabc3582]	PubMed: 32404436
Androgen Signaling Regulates SARS-CoV-2 Receptor Levels and Is Associated with Severe COVID-19 Symptoms in Men [ Cell Stem Cell, 2020, 27(6):876-889.e12]	PubMed: 33232663

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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