Camostat Mesilate 化学構造
分子量: 494.52

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Quality Control & MSDS

製品説明

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製品の説明

生物活性

製品説明 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.
ターゲット Matriptase Human neutrophil elastase
IC50 0.5 μM 0.2 μM [1]
In vitro試験 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試験 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]
臨床試験
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

Binding assay 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: [2]

動物モデル male Wistar rats
製剤 Saline
投薬量 2 mg/g
投与方法 Diet

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Camostat Mesilate SDF
分子量 494.52
化学式

C20H22N4O5.CH4O3S

CAS No. 59721-29-8
保管 2年-20℃
6月-80℃in solvent
別名 FOY-305
溶解度 (25°C) * In vitro DMSO 99 mg/mL (200.19 mM)
10 mg/mL (20.22 mM)
エタノール <1 mg/mL (<1 mM)
* <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.
化学名 Benzeneacetic acid, 4-[[4-[(aminoiminomethyl)amino]benzoyl]oxy]-, 2-(dimethylamino)-2-oxoethyl ester, methanesulfonate (1:1)

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