Bioactivity | Antitrypanosomal agent 1 is a potent and selective trypanothione reductase (TR) inhibitor with an IC50 of 3.3 μM. Antitrypanosomal agent 1 inhibits glutathione reductase (GR) (IC50=64.8 μM) and T. brucei (EC50=1 μM). Antitrypanosomal agent 1 has anti-trypanosomal activity[1]. |
Target | IC50: 3.3 μM (trypanothione reductase) and 64.8 μM (glutathione reductase)EC50: 1 μM (T. brucei) |
Invitro | Antitrypanosomal agent 1 (compound 8a) has an selectivity for TR (GR IC50/TR IC50) of 20[1]. |
Name | Antitrypanosomal agent 1 |
CAS | 75144-12-6 |
Formula | C11H14Cl3NO |
Molar Mass | 282.59 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
Reference | [1]. Martyn DC, et al. High-throughput screening affords novel and selective trypanothione reductase inhibitors with anti-trypanosomal activity. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1280-3. |