 
        
        
        
                货号:A238171
                
                同义名:
                    
                        
                            卡莫他特甲磺酸盐
                            
                             / Camostat mesilate; FOY305
                            
                        
                    
                
                
                
                    
                     
                
            
Camostat Mesylate是一种丝氨酸蛋白酶抑制剂 (IC50 = 50 nM),可抑制 TMPRSS2 和胰蛋白酶活性,对 SARS-CoV-2 具有抗病毒活性,广泛用于炎症和传染病研究。
 HazMat Fee +
 HazMat Fee + There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
| Type | HazMat fee for 500 gram (Estimated) | 
| Excepted Quantity | USD 0.00 | 
| Limited Quantity | USD 15-60 | 
| Inaccessible (Haz class 6.1), Domestic | USD 80+ | 
| Inaccessible (Haz class 6.1), International | USD 150+ | 
| Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ | 
| Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ | 
 
                                 
                                
                            

| 规格 | 价格 | 会员价 | 库存 | 数量 | |||
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| 产品名称 | Sodium Channel ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Tolperisone HCl | ✔ | 99% | |||||||||||||||||
| Triamterene | +++ ENaC, IC50: 4.5 μM | 98% | |||||||||||||||||
| Lamotrigine | ✔ | 98% | |||||||||||||||||
| Vinpocetine | ✔ | 98% | |||||||||||||||||
| Zonisamide | ✔ | 99% | |||||||||||||||||
| Dronedarone HCl | ✔ | 95% | |||||||||||||||||
| Procainamide HCl | ✔ | 99% | |||||||||||||||||
| Bupivacaine HCl | ✔ | 99+% | |||||||||||||||||
| Benzocaine | ✔ | 98% | |||||||||||||||||
| Carbamazepine | ++ Sodium channel, IC50: 131 μM | 98% | |||||||||||||||||
| Quinidine sulfate dihydrate | ✔ | 98% | |||||||||||||||||
| Ibutilide fumarate | ✔ | 99%+ | |||||||||||||||||
| Dibucaine HCl | ✔ | 99+% | |||||||||||||||||
| Mexiletine HCl | ✔ | 99% | |||||||||||||||||
| Phenytoin | ✔ | 99+% | |||||||||||||||||
| Camostat Mesylate | +++ epithelial sodium channel (ENaC), IC50: 50 nM | 99%+ | |||||||||||||||||
| Levobupivacaine | ✔ | 97+% | |||||||||||||||||
| Oxcarbazepine | + sodium channel, IC50: 160 μM | 98% | |||||||||||||||||
| Amiloride HCl dihydrate | ✔ | 97% | |||||||||||||||||
| Ambroxol | 98+% | ||||||||||||||||||
| Primidone | ✔ | 99% | |||||||||||||||||
| Propafenone | ✔ | 99% | |||||||||||||||||
| A-803467 | ++++ Na(V1.8) channel, IC50: 8 nM | 99%+ | |||||||||||||||||
| Rufinamide | ✔ | 99% | |||||||||||||||||
| Phenytoin sodium | ✔ | 98% | |||||||||||||||||
| Proparacaine HCl | + Voltage-gated sodium channel, ED50: 3.4 mM | 98+% | |||||||||||||||||
| Amiloride HCl | ✔ | 98% | |||||||||||||||||
| Riluzole | ✔ | 97% | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 靶点 | 
 | 
| 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]. | 
| Concentration | Treated Time | Description | References | |
| PK | 10.4 nM (IC50) | Determination of Camostat's inhibitory effect on PK, IC50 of 10.4 nM | J Virol. 2021 Sep 9;95(19):e0086121. | |
| HEK-293T | 142 nM (IC50) | Confirm Camostat inhibits TMPRSS2 activity | Chem Sci. 2020 Nov 13;12(3):983-992. | |
| Cathepsin G (CatG) | 80 µg/mL | 1 hour | Analyze the inhibitory capacity of camostat towards CatG proteolytic activity | Pharmaceuticals (Basel). 2022 Apr 20;15(5):500. | 
| Proteinase 3 (PR3) | 0 to 1000 µM | 15 minutes | Analyze the inhibitory capacity of camostat towards PR3 proteolytic activity | Pharmaceuticals (Basel). 2022 Apr 20;15(5):500. | 
| Proteinase 3 (PR3) | 40 µg/mL | 15 minutes | Analyze the inhibitory capacity of camostat towards PR3 proteolytic activity | Pharmaceuticals (Basel). 2022 Apr 20;15(5):500. | 
| Neutrophil Elastase (NE) | 40 µg/mL | 15 minutes | Analyze the inhibitory capacity of camostat towards NE proteolytic activity | Pharmaceuticals (Basel). 2022 Apr 20;15(5):500. | 
| Calu-3 cells | 0.01, 0.1, 1, 10, 100 µM | 2 hours | Evaluate the inhibitory effect of Camostat mesylate on SARS-2-S-driven cell entry | EBioMedicine. 2021 Mar;65:103255. | 
| BHK-21 cells | 100 µM | 2 hours | Evaluate the inhibitory effect of Camostat mesylate on SARS-2-S-driven cell entry | EBioMedicine. 2021 Mar;65:103255. | 
| Primary human lung cells | 1-500 µM | 2 hours pretreatment | To evaluate the importance of TMPRSS2 for SARS-2-S-driven cell entry, camostat mesylate significantly reduced SARS-2-S-driven entry | Cell. 2020 Apr 16;181(2):271-280.e8. | 
| Calu-3 cells | 1-500 µM | 2 hours pretreatment | To evaluate the importance of TMPRSS2 for SARS-2-S-driven cell entry, camostat mesylate significantly reduced SARS-2-S-driven entry | Cell. 2020 Apr 16;181(2):271-280.e8. | 
| Vero-TMPRSS2 cells | 1-500 µM | 2 hours pretreatment | To evaluate the importance of TMPRSS2 for SARS-2-S-driven cell entry, camostat mesylate partially blocked SARS-2-S-driven entry | Cell. 2020 Apr 16;181(2):271-280.e8. | 
| Caco-2 cells | 1-500 µM | 2 hours pretreatment | To evaluate the importance of TMPRSS2 for SARS-2-S-driven cell entry, camostat mesylate partially blocked SARS-2-S-driven entry | Cell. 2020 Apr 16;181(2):271-280.e8. | 
| Trypsin | 9.3 nM (IC50) | Determination of Camostat's inhibitory effect on trypsin, IC50 of 9.3 nM | J Virol. 2021 Sep 9;95(19):e0086121. | |
| Matriptase | 21.1 nM (IC50) | Determination of Camostat's inhibitory effect on matriptase, IC50 of 21.1 nM | J Virol. 2021 Sep 9;95(19):e0086121. | |
| FXIa | 44.1 nM (IC50) | Determination of Camostat's inhibitory effect on FXIa, IC50 of 44.1 nM | J Virol. 2021 Sep 9;95(19):e0086121. | |
| MuPA | 100.4 nM (IC50) | Determination of Camostat's inhibitory effect on muPA, IC50 of 100.4 nM | J Virol. 2021 Sep 9;95(19):e0086121. | |
| UPA | 86.4 nM (IC50) | Determination of Camostat's inhibitory effect on uPA, IC50 of 86.4 nM | J Virol. 2021 Sep 9;95(19):e0086121. | |
| Administration | Dosage | Frequency | Description | References | ||
| Mice | Pancreatic growth model | Oral | 400 mg/kg/day | Once daily for 10 days | To assess the effects of camostate on pancreatic growth and plasma CCK concentration in mice. The results showed that chronic camostate feeding significantly increased pancreatic weight, protein and DNA content, and markedly elevated plasma CCK concentration. | Gut. 1987;28 Suppl(Suppl):63-9 | 
| 计算器 | ||||
| 存储液制备 |  | 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 | |
| CAS号 | 59721-29-8 | 
| 分子式 | C21H26N4O8S | 
| 分子量 | 494.52 | 
| SMILES Code | O=C(OCC(N(C)C)=O)CC1=CC=C(OC(C2=CC=C(NC(N)=N)C=C2)=O)C=C1.CS(=O)(O)=O | 
| MDL No. | MFCD00941410 | 
| 别名 | 卡莫他特甲磺酸盐 ;Camostat mesilate; FOY305; Foipan; Camostat (mesylate); FOY-S980 | 
| 运输 | 蓝冰 | 
| InChI Key | FSEKIHNIDBATFG-UHFFFAOYSA-N | 
| Pubchem ID | 5284360 | 
| 存储条件 | In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, room temperature | 
| 溶解方案 | 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) 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 
 
 
 
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