Atrasentan hydrochloride

Research use only, not for human use.

Atrasentan hydrochloride is an antagonist of the endothelin receptor(IC50 = 55.1 μM for ETA).

Atrasentan hydrochloride is an antagonist of the endothelin receptor(IC50 = 55.1 μM for ETA).(In Vitro):Atrasentan hydrochloride (0-50 μM) significantly inhibits LNCaP and C4-2b prostate cancer cell growth. ABT-627 in combination with Taxotere elicits a significantly greater loss of viable prostate cancer cells relative to either agent alone and shows a greater degree of down-regulation of the NF-κB DNA binding activity . Atrasentan hydrochloride profoundly induces several CYPs and drug transporters. It is a moderate P-gp inhibitor (IC50 = 15.1 μM in P388/dx cells) and a weak BCRP inhibitor (IC50 = 59.8 μM in MDCKII-BCRP cells) .(In Vivo):Atrasentan hydrochloride (10 mg/kg, i.p.) inhibited the C4-2b tumor growth within the bone environment to some extent in the SCID-hu model . Atrasentan hydrochloride (3 mg/kg, p.o.) inhibits the pressor response induced by big endothelin-1 (1 nmol/kg) in pithed rats .

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

GPCR/G Protein

Endothelin Receptor

Endothelin Receptor

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195733-43-8

547.09

C29H39ClN2O6

>98% (HPLC)

In Vitro:?DMSO : 28.57 mg/mL (52.22 mM)

Cl.CCCCN(CCCC)C(=O)CN1CC(C(C1c1ccc(OC)cc1)C(O)=O)c1ccc2OCOc2c1

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(-20℃)

With Ice Pack

≥ 2 years