For research use only. Not for therapeutic Use.
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].
Gallinamide A TFA has low cytotoxicity with CC50 >100 μM in VeroE6 cells. Gallinamide A TFA (0.5 μM; 96 h) can inhibit CatL-mediated SARS-CoV-2 endosome entry into VeroE6 cells[1].Gallinamide A TFA also mesylate with the TMPRSS2 inhibitor Nafamostat (HY-B0190A) exhibits synergistic effects. Potent antiviral activity in HEK-ACE2-TMPRSS2 cells, but ineffective in VeroE6 cell line[1].
| Catalog Number | I040006 |
| CAS Number | 1352920-57-0 |
| Synonyms | [(2S)-1-[[(2S)-1-[[(E,2S)-5-[(2S)-3-methoxy-2-methyl-5-oxo-2H-pyrrol-1-yl]-5-oxopent-3-en-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl] (2S,3S)-2-(dimethylamino)-3-methylpentanoate;2,2,2-trifluoroacetic acid |
| Molecular Formula | C33H53F3N4O9 |
| Purity | ≥95% |
| InChI | InChI=1S/C31H52N4O7.C2HF3O2/c1-12-20(6)28(34(9)10)31(40)42-25(16-19(4)5)30(39)33-23(15-18(2)3)29(38)32-21(7)13-14-26(36)35-22(8)24(41-11)17-27(35)37;3-2(4,5)1(6)7/h13-14,17-23,25,28H,12,15-16H2,1-11H3,(H,32,38)(H,33,39);(H,6,7)/b14-13+;/t20-,21-,22-,23-,25-,28-;/m0./s1 |
| InChIKey | LSQVWYLBGSKLOU-VXEXLYRGSA-N |
| SMILES | CCC(C)C(C(=O)OC(CC(C)C)C(=O)NC(CC(C)C)C(=O)NC(C)C=CC(=O)N1C(C(=CC1=O)OC)C)N(C)C.C(=O)(C(F)(F)F)O |
| 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. |
