产品说明书
PF-07321332
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同义名 : | - |
| CAS号 : | 2628280-40-8 | |
| 货号 : | A1462928 | |
| 分子式 : | C23H32F3N5O4 | |
| 纯度 : | 98% | |
| 分子量 : | 499.526 | |
| MDL号 : | - | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 135 mg/mL(270.26 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 无水乙醇: 50 mg/mL(100.09 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is the cause of the COVID-19 pandemic. The coronavirus 3-chymotrypsin-like protease (3CLpro) controls virus replication and is therefore considered a major target and promising opportunity for rational-based antiviral discovery with direct acting agents[1]. PF-07321332 is an oral antiviral SARS-CoV-2-3CL protease inhibitor[2]. The hydrogen bonds formed by lopinavir and ritonavir with 3CLpro are inconsistent and weak as compared with the interactions of 3CLpro with PF-07321332 and α-ketoamide. PF-07321332 showed more considerable binding energy toward 3CLpro, almost by 28 kJ/mol, and three times more than lopinavir and ritonavir. The interaction of PF-07321332 and α-ketoamide with the catalytic site residues may cause the distortion of the oxyanion hole in the reaction mechanism, and it may lead to the inhibition of 3CLpro in SARS-CoV-2. Compared with PF-07321332 and α-ketoamide, both antiretroviral drugs lopinavir and ritonavir manifested weaker interactions with 3CLpro, judging by binding energy values[3]. PF-07321332 was strongly bonded to 3CLpro and capable to disrupt the His41–Cys145 catalytic dyad, which, together with the N-terminus residues 1 to 7, is thought to have a vital role in proteolytic activity[4]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.00mL 0.40mL 0.20mL |
10.01mL 2.00mL 1.00mL |
20.02mL 4.00mL 2.00mL |
| 参考文献 |
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