Gallinamide A TFA
Based on 1 Customer Validation
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).
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- Pureté : 99.85%
- CAS No.: 1352920-57-0
- Formule: C33H53F3N4O9
- Masse moléculaire:706.79
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Stockage:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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Activité biologique
Description
IC50 & 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)[1]
EC50: 28 nM (SARS-CoV-2)[1]
IC50: 50 nM (P. falciparum)[2]
In Vitro
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1352920-57-0
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Appearance Solid
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Masse moléculaire 706.79
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Formule C33H53F3N4O9
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Color White to off-white
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SMILES
CC[C@H](C)[C@H](N(C)C)C(O[C@@H](CC(C)C)C(N[C@@H](CC(C)C)C(N[C@@H](C)/C=C/C(N1[C@H](C(OC)=CC1=O)C)=O)=O)=O)=O.OC(C(F)(F)F)=O
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Structure Classification
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Initial Source
marine cyanobacterium Schizothrix sp.
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Pureté et documentation
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Fiche technique (269 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)