MM3122 是一种选择性的 II 型跨膜丝氨酸蛋白酶 (TMPRSS2) 抑制剂,IC50为 0.34 nM。MM3122 可以有效阻断 TMPRSS2,从而抑制 SARS-CoV-2 和 MERS-CoV 进入人类细胞。
产品描述
MM3122 is a selective type II transmembrane serine protease (TMPRSS2) inhibitor, IC50 = 0.34 nM. MM3122 effectively blocks TMPRSS2, thereby inhibiting the entry of SARS-CoV-2 and MERS-CoV into human cells.
体外活性
MM3122 (0-1 μM) has inhibitory activity against HGFA, matriptase, hepsin and thrombin with the IC50 values of 32, 0.31, 0.19 and more than 20 nM, respectively. MM3122 (0.1-100 μM) inhibits SARS-CoV-2 calu-3, MERS VSV pseudotype calu-3 and VSV-SARS CoV-2 chimera calu-3 with the EC50 values of 74, 0.87 nM and 0.43 respectively [1].
体内活性
MM3122 (i.p., 0-100 mg/kg, daily, 7 days) has no adverse effects, no weight loss or changes in harvested organs (liver, spleen and kidney) compared to controls. MM3122 (i.p., 16.7 mg/kg, once) has a half-life of 8.6 hours in plasma and 7.5 hours in lung of NSG mice[1].
Cas No.
2574390-27-3
分子式
C31H39N9O6S
分子量
665.76
别名
GTPL11533;MM-3122;Ac-GQFR-kbt
储存和溶解度
DMSO:90 mg/mL (135.2 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years