Genz 669178
Names
[ CAS No. ]:
1254834-91-7
[ Name ]:
Genz 669178
[Synonym ]:
5-(4-Cyano-2-methyl-1H-benzimidazol-1-yl)-N-cyclopropyl-2-thiophenecarboxamide
5-(4-Cyano-2-Methyl-1h-Benzimidazol-1-Yl)-N-Cyclopropylthiophene-2-Carboxamide
2-Thiophenecarboxamide, 5-(4-cyano-2-methyl-1H-benzimidazol-1-yl)-N-cyclopropyl-
Biological Activity
[Description]:
A potent PfDHODH inhibitor that exhibits low nanomolar in vitro potency against DHODH from P falciparum, P vivax, and P berghei; demonstrates in vitro potency against the 3D7 and Dd2 strains of P. falciparum, good tolerability and oral exposure in the mouse, and ED(50) values in the 4-day murine P. berghei efficacy model of 13-21 mg/kg/day with oral twice-daily dosing.
[References]
References 1. Lukens AK, e tal. Proc Natl Acad Sci U S A. 2014 Jan 14;111(2):799-804. 2. Booker ML, et al. J Biol Chem. 2010 Oct 22;285(43):33054-64. 3. Skerlj RT, et al. ACS Med Chem Lett. 2011 Jul 11;2(9):708-13. View Related Products by Target Bacterial
Chemical & Physical Properties
[ Density]:
1.5±0.1 g/cm3
[ Molecular Formula ]:
C17H14N4OS
[ Molecular Weight ]:
322.384
[ Exact Mass ]:
322.088837
[ LogP ]:
2.17
[ Index of Refraction ]:
1.766