Atrasentan (hydrochloride)

195733-43-8

C29H39ClN2O6

DMSO : >= 33.3 mg/mL (60.87 mM)

GPCR/G Protein

Atrasentan (hydrochloride) is an endothelin receptor antagonist with IC₅₀ of 0.0551 nM for ET_A. IC50 & Target: IC50: 0.055 nM (ET_A) In Vitro: Atrasentan (ABT-627, 0-50 uM) significantly inhibits LNCaP and C4-2b prostate cancer cell growth. ABT-627 in conbination with Taxotere elicits a significantly greater loss of viable prostate cancer cells relative to either agent alone and shows greater degree of down-regulation of the NF-kappaB DNA binding activity^[2]. Atrasentan profoundly induces several CYPs and drug transporters (e.g. 12-fold induction of CYP3A4 at 50 uM). It is a moderate P-gp inhibitor (IC₅₀ in P388/dx cells=15.1+/-1.6 uM) and a weak BCRP inhibitor (IC₅₀ in MDCKII-BCRP cells=59.8+/-11 uM)^[3]. In Vivo: Atrasentan (3 mg/kg, p.o.) inhibits the pressor response induced by big endothelin-1 (1 nmol/kg) in pithed rats^[1]. Aatrasentan (ABT-627, 10 mg/kg, i.p.) as well as Taxotere alone inhibited the C4-2b tumor growth within the bone environment to some extent in the SCID-hu model^[2].