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Atrasentan

Chemical Structure : Atrasentan

CAS No.: 173937-91-2

Atrasentan (ABT-627, ABT627, A-147627)

Catalog No.: PC-21324Not For Human Use, Lab Use Only.

Atrasentan (ABT-627, A-147627) is a potent, selective and orally active nonpeptide endothelin A-receptor (ETA) with IC50 of 0.055 nM.

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Biological Activity

Atrasentan (ABT-627, A-147627) is a potent, selective and orally active nonpeptide endothelin A-receptor (ETA) with IC50 of 0.055 nM.
Atrasentan (ABT-627, A-147627) significantly inhibits LNCaP and C4-2b prostate cancer cell growth.
Atrasentan (ABT-627, A-147627) inhibits ET-1 radioligand binding with IC50 of 0.36 nM, 1000-fold selectivity for the ET(A) vs the ET(B) receptor.
Atrasentan (ABT-627, A-147627) also is a potent inhibitor (IC50=0.16 nM) of phosphoinositol hydrolysis stimulated by ET-1, and it antagonizes the ET-1-induced contraction of the rabbit aorta with a pA(2)=9.20.

Physicochemical Properties

M.Wt 510.63
Formula C29H38N2O6
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2r,3r,4s)-4-(benzo[d][1,3]dioxol-5-yl)-1-(2-(dibutylamino)-2-oxoethyl)-2-(4-methoxyphenyl)pyrrolidine-3-carboxylicacid

References

1. Winn M, et al. J Med Chem. 1996 Mar 1;39(5):1039-48.

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