orteronel-racemic

Description: Orteronel racemate, the mixture of S-enantiomer and R-enantiomer of Orteronel (aslo known as TAK-700) which is a novel, potent and highly selective, orally bioavailable non-steroidal androgen synthesis inhibitor of human 17, 20-lyase inhibitor with IC50 of 38 nM, it exhibits > 1000-fold selectivity over other CYPs (e.g. 11-hydroxylase and CYP3A4). TAK-700 has potential antiandrogen activity by binding to and inhibiting the steroid 17alpha-monooxygenase in both the testes and adrenal glands, thereby inhibiting androgen production. This may decrease androgen-dependent growth signaling and may inhibit cell proliferation of androgen-dependent tumor cells.

References: Bioorg Med Chem. 2011 Nov 1; 19(21):6383-99; J Steroid Biochem Mol Biol. 2012 Apr; 129(3-5):115-28.

Related CAS : 426219-18-3 (racemate); 566939-85-3 (s-isomer)