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Atrasentan (hydrochloride)


CAS No. : 195733-43-8

(Synonyms: ABT-627 (hydrochloride); (+)-A 127722 (hydrochloride); A-147627 (hydrochloride))

195733-43-8
Price and Availability of CAS No. : 195733-43-8
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Cat. No. : HY-15403A
M.Wt: 547.08
Formula: C29H39ClN2O6
Purity: >98 %
Solubility: DMSO : 28.57 mg/mL (ultrasonic);H2O : 0.5 mg/mL (ultrasonic;warming;adjust pH to 4 with HCl;heat to 60°C);0.1 M HCL : < 1 mg/mL (ultrasonic;warming;adjust pH to 1 with HCl;heat to 60°C)
Introduction of 195733-43-8 :

Atrasentan hydrochloride (ABT-627 hydrochloride) is a selective endothelin A receptor antagonist with an IC50 of 0.0551 nM for ETA[1]. IC50 & Target:IC50: 0.055 nM (ETA) In Vitro:Atrasentan hydrochloride (ABT-627 hydrochloride) (0-50 μM) significantly inhibits LNCaP and C4-2b prostate cancer cell growth[2]. 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)[3]. In Vivo:Atrasentan hydrochloride (ABT-627 hydrochloride) (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.) inhibits the C4-2b tumor growth within the bone environment to some extent in the SCID-hu model[2].

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