Atrasentan

Research use only, not for human use.

Atrasentan (ABT-627) is an endothelin receptor antagonist (IC50: 0.0551 nM for ETA).

Atrasentan (ABT-627) is an endothelin receptor antagonist (IC50: 0.0551 nM for ETA).

Atrasentan (ABT-627, 0-50 μM) 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-κB DNA binding activity. Atrasentan profoundly induces several CYPs and drug transporters (e.g. 12-fold induction of CYP3A4 at 50 μM). It is a moderate P-gp inhibitor (IC50 in P388/dx cells=15.1±1.6 μM) and a weak BCRP inhibitor (IC50 in MDCKII-BCRP cells=59.8±11 μM).

Atrasentan (3 mg/kg, p.o.) inhibits the pressor response induced by big endothelin-1 (1 nmol/kg) in pithed rats. 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.

ABT-627 | (+)-A 127722 | A-147627

GPCR/G Protein

Endothelin Receptor

ET-A

——

——

173937-91-2

510.62

C29H38N2O6

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (184.27 mM)

CCCCN(CCCC)C(CN(C[C@@H]([C@H]1C(O)=O)c(cc2)cc3c2OCO3)[C@H]1c(cc1)ccc1OC)=O

——

(-20℃)

With Ice Pack

≥ 2 years