Other Biochemicals - Atrasentan hydrochloride (CAS: 195733-43-8)

Atrasentan hydrochloride (CAS: 195733-43-8)

Catalog #：EBC51035

Biological Activity

Synonyms

ABT-627 hydrochloride, ABT627 hydrochloride, ABT 627 hydrochloride, Abbott 147627 hydrochloride

Chemical Name

(2R,3R,4S)-4-(1,3-Benzodioxol-5-yl)-1-2-(dibutylamino)-2-oxoethyl-2-(4-methoxyphenyl)-3-pyrrolidinecarboxylic acid hydrochloride

Application

Atrasentan hydrochloride is an endothelin receptor antagonist

CAS Number

195733-43-8

Purity

≥99.0%

Molecular Weight

547.08

Molecular Formula

C₂₉H₃₉ClN₂O₆

SMILES

CCCCN(CCCC)C(=O)CN1C[C@@H]([C@H]([C@@H]1C2=CC=C(C=C2)OC)C(=O)O)C3=CC4=C(C=C3)OCO4.Cl

Target & IC50

Endothelin Receptor Antagonist :IC50 =0.055 nM

Shipping

Gel Pack

Storage

Store at -20°C

Preparing Stock Solutions

Molecular Structure

ConcentrationSolventMass	1 mg	5 mg	10 mg
1 mM	1.8279 ml	9.1394 ml	18.2789 ml
5 mM	0.3656 ml	1.8279 ml	3.6558 ml
10 mM	0.1828 ml	0.9139 ml	1.8279 ml
50 mM	0.0366 ml	0.1828 ml	0.3656 ml

Solubility
DMSO: 30 mg/mL (54.84 mM)

Product Description

Atrasentan Hcl(A-147627) is an endothelin antagonist receptor (IC50=0.0551 nM, ETA) being developed for the treatment of prostate cancer.

In vitro: The combination of Atrasentan with Taxotere was more effective in the inhibition of cell viability and induction of apoptosis in LNCaP and C4-2b cells (androgen receptor positive) but not in PC-3 cells. Atrasentan profoundly induced several CYPs and drug transporters (e.g. 12-fold induction of CYP3A4 at 50 μM). It was a moderate P-gp inhibitor (IC(50) in P388/dx cells = 15.1 ± 1.6 μM) and a weak BCRP inhibitor (IC(50) in MDCKII-BCRP cells = 59.8 ± 11 μM). BCRP or P-gp overexpressing cells were slightly more resistant towards antiproliferative effects of atrasentan .

In vivo: ABT-627 did reduce the accumulation of macrophages in both stains (36 to 53%) whereas it blocked by 76% the influx of eosinophils in Balb/c but not in C57Bl/6 mice. Atrasentan was administered orally via drinking water at 3 mg kg-1 per day over 28 days. All diabetic mice developed similar hyperglycaemia (27-30 mmol l-1). Atrasentan treatment significantly improved left ventricular systolic and diastolic function in response to exogenous norepinephrine, but there were no differences between genotypes.