| Bioactivity | Gallinamide A TFA is a linearly depositing peptide and a potent inhibitor of cathepsin L (CatL) (IC50: 17.6 pM). Gallinamide A TFA inhibits SARS-CoV-2 infection by inhibiting CatL (EC50: 28 nM). Gallinamide A TFA also inhibits Plasmodium falciparum (IC50: 50 nM)[1][2]. |
| Target | IC50: 17.6 pM (Cathepsin L); 7.34 nM (Cathepsin B); 697 nM (Cathepsin V); 79.6 nM (Cathepsin K); 367 pM (Cathepsin S)EC50: 28 nM (SARS-CoV-2)IC50: 50 nM (P. falciparum) |
| Invitro | Gallinamide A TFA 对细胞毒性低，对 VeroE6 细胞的 CC50 >100 μM。Gallinamide A TFA (0.5 μM; 96 h) 可以通过抑制 CatL 介导的 SARS-CoV-2 内体进入 VeroE6 细胞[1].Gallinamide A TFA 还与 TMPRSS2 抑制剂 Nafamostat mesylate (HY-B0190A) 表现出协同作用。在 HEK-ACE2-TMPRSS2 细胞中具有有效的抗病毒活性，但在 VeroE6 细胞系中无效[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Gallinamide A TFA 相关抗体: |
| CAS | 1352920-57-0 |
| Formula | C33H53F3N4O9 |
| Molar Mass | 706.79 |
| Appearance | 固体 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen) |
| Reference | [1]. Ashhurst AS, et al. Potent in vitro anti-SARS-CoV-2 activity by gallinamide A and analogues via inhibition of cathepsin L. bioRxiv [Preprint]. 2020 Dec 24:2020.12.23.424111. [2]. Stoye A, et al. Falcipain Inhibitors Based on the Natural Product Gallinamide A Are Potent in Vitro and in Vivo Antimalarials. J Med Chem. 2019 Jun 13;62(11):5562-5578. |
Gallinamide A TFA
CAS: 1352920-57-0 F: C33H53F3N4O9 W: 706.79
Gallinamide A TFA is a linearly depositing peptide and a potent inhibitor of cathepsin L (CatL) (IC50: 17.6 pM). Gallina
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