Camostat Mesylate

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Chemical Structure| 59721-29-8 同义名 : 卡莫他特甲磺酸盐 ;Camostat mesilate;FOY305;Foipan;Camostat (mesylate);FOY-S980
CAS号 : 59721-29-8
货号 : A238171
分子式 : C21H26N4O8S
纯度 : 99%+
分子量 : 494.518
MDL号 : MFCD00941410
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(242.66 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(101.11 mM)
动物实验配方：
生物活性
靶点

  • Sodium Channel

    epithelial sodium channel (ENaC), IC50:50 nM
描述 Camostat mesylate (CM) is a trypsin-like protease inhibitor, inhibits airway epithelial sodium channel (ENaC) function with IC50 of 50 nM, less potent to trypsin, prostasin and matriptase. It also inhibits transmembrane serine protease TMPRSS2, suggesting that it could block entry of SARS-Cov-2 (COVID-19) into lung cells in vitro[3]. In vivo, the oral administration of CM inhibited inflammation, cytokines expression and fibrosis in the pancreas. CM inhibited both MCP-1 (monocyte chemoattractant protein-1) and TNF-alpha production from monocytes, and proliferation and MCP-1 production from PSCs (panceatic stellate cells) [4]. Camostat mesilate (30 mg/kg; p.o.; twice a day for 9 days) blocks the spread and pathogenesis of SARS-CoV in a pathogenic mouse model[5]. CM alleviated the detrimental effect of LPS on cell viability and inhibited LPS-induced TNF-α and IL-6 secretions in DF-1 chicken embryo fibroblasts[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.02mL

0.40mL

0.20mL

10.11mL

2.02mL

1.01mL

20.22mL

4.04mL

2.02mL
参考文献

[1]Coote K, Atherton-Watson HC, et al. Camostat attenuates airway epithelial sodium channel function in vivo through the inhibition of a channel-activating protease. J Pharmacol Exp Ther. 2009 May;329(2):764-74.

[2]Okuno M, Akita K, et al. Prevention of rat hepatic fibrosis by the protease inhibitor, camostat mesilate, via reduced generation of active TGF-beta. Gastroenterology. 2001 Jun;120(7):1784-800.

[3]Coote K, Atherton-Watson HC, Sugar R, Young A, MacKenzie-Beevor A, Gosling M, Bhalay G, Bloomfield G, Dunstan A, Bridges RJ, Sabater JR, Abraham WM, Tully D, Pacoma R, Schumacher A, Harris J, Danahay H. Camostat attenuates airway epithelial sodium channel function in vivo through the inhibition of a channel-activating protease. J Pharmacol Exp Ther. 2009 May;329(2):764-74

[4]Gibo J, Ito T, Kawabe K, Hisano T, Inoue M, Fujimori N, Oono T, Arita Y, Nawata H. Camostat mesilate attenuates pancreatic fibrosis via inhibition of monocytes and pancreatic stellate cells activity. Lab Invest. 2005 Jan;85(1):75-89

[5]Zhou Y, Vedantham P, Lu K, Agudelo J, Carrion R Jr, Nunneley JW, Barnard D, Pöhlmann S, McKerrow JH, Renslo AR, Simmons G. Protease inhibitors targeting coronavirus and filovirus entry. Antiviral Res. 2015 Apr;116:76-84

[6]Yuan L, Li M, Zhang Z, Li W, Jin W, Wang M. Camostat mesilate inhibits pro-inflammatory cytokine secretion and improves cell viability by regulating MFGE8 and HMGN1 in lipopolysaccharide-stimulated DF-1 chicken embryo fibroblasts. PeerJ. 2021 Aug 26;9:e12053