Shelf life (days): 1460.0
Formulation: A solid
Formal Name: 4-(1,3-benzodioxol-5-yl)-1-[2R-(dibutylamino)-2-oxoethyl]-2-(4S-methoxyphenyl)-3R-pyrrolidinecarboxylic acid, monohydrochloride
Purity: ≥98%
Formula Markup: C29H38N2O6 / HCl
Formula Weight: 547.1
CAS Number: 195733-43-8
Notes: Atrasentan is an antagonist of endothelin receptor type A (ETA; Ki = 69 pM for the human receptor).{51849} It is selective for ETA over ETB (Ki = 139 nM for the human receptor) and a panel of 29 other receptors at 10 µM. Atrasentan inhibits endothelin-1-induced secretion of arachidonic acid (Item Nos. 90010 / 90010.1 / 10006607) from human pericardial smooth muscle cells (HPSMCs; pA2 = 10.5), as well as endothelin-1-induced vasoconstriction in isolated rat aortic rings (pA2 = 9.2). It inhibits endothelin-1-induced increases in the pressor response in normotensive rats when administered at a dose of 10 mg/kg. Atrasentan (5 mg/kg per day) reduces urinary levels of albumin, TGF-β, and a prostaglandin E2 metabolite, as well as decreases the number of macrophages in the renal cortex, in a rat model of streptozotocin-induced diabetic nephropathy.{51850}
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