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Antitrypanosomal agent 1

CAS: 75144-12-6 F: C11H14Cl3NO W: 282.59

Antitrypanosomal agent 1 is a potent and selective trypanothione reductase (TR) inhibitor with an IC50 of 3.3 μM. Antit
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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.