Atrasentan

Product details

• Chemical name: (2R,3R,4S)-4-(1,3-benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-(4-methoxyphenyl)pyrrolidine-3-carboxylic acid.
• Also known as: (+)-A-127722, A-147627, ABT-627
• CAS number: 173937-91-2
• Molecular formula: C29H38N2O6.
• Purity: >98%
• Concentration: 0.01-10 nM.
• Form: Lyophilized powder.
• Solubility: Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
• Reconstitution: Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
• Shipping: Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
• Target: ET-A receptors
• Source: Synthetic
• Activity: Atrasentan is a potent and highly selective antagonist of ET-A endothelin receptors, exhibiting a 1000-fold selectivity for ET-A over ET-B receptors, inhibiting endothelin-1 radioligand binding with an IC50 of 0.36 nM and endothelin-1-stimulated phosphoinositol hydrolysis with IC50 of 0.16 nM1.
• Alternative names: (+)-A-127722, A-147627, ABT-627

Scientific background

Atrasentan (A-127722) is a synthetic compound that acts as a potent and selective antagonist of endothelin A (ET-A) receptor. Atrasentan is highly selective towards ET-A receptor, exhibiting 1000-fold selectivity over ET-B receptors1. It inhibits endothelin-1 radioligand binding with an IC50 value of 0.36 nM and endothelin-1-stimulated phosphoinositol hydrolysis with an IC50 of 0.16 nM1.ET-A receptors are predominantly detected in peripheral tissues, especially in vascular smooth muscle tissues where they mediate vasoconstriction. They are also expressed in several regions of the brain. The ET-A receptor has high affinity for endothelin-1 and endothelin-2 and relatively low affinity for endothelin-3, while the ET-B receptor has high affinity for all endothelin isopeptides2.

Lead time: 1-2 Business Days

Country of origin: Israel/IL

Applications key

Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.

Bioassay tested: Yes

• SDS (PDF)

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