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Atrasentan hydrochloride (CAS: 195733-43-8)
Catalog #£ºEBC51035
  SKU-Pack Size Availability Size Price
EBC51035-1ML In Stock 1mL(10mM in DMSO) €479.70
EBC51035-5MG In Stock 5mg €219.70
EBC51035-10MG In Stock 10mg €349.70
EBC51035-25MG In Stock 25mg €479.70
EBC51035-50MG In Stock 50mg €609.70
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Product Information
Synonym(s) 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 ¡Ý99.0%
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
Solubility DMSO: 30 mg/mL (54.84 mM)
Preparing Stock Solutions
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
Shipping Gel Pack
Storage Store at -20¡ãC
Research Use For Research Use Only. Not Intended for Diagnostic Or Therapeutic Use.
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.

Specific Protocols
>> Western Blotting Protocol >> Immunoprecipitation Protocol
>> Immunohistochemistry Protocol >> Immunofluorescence Protocol
>> Immunocytochemistry Protocol >> Flow Cytometry Protocol
>> ChIP Protocol >> ELISA Protocol
>> HPLC Protocol >> PCR Protocol
For Research Use Only, Not For Diagnostic Or Therapeutic Procedures.
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