An ETA antagonist
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Atrasentan (hydrochloride)

Item No. 31238

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(1,3-benzodioxol-5-yl)-1-[2R-(dibutylamino)-2-oxoethyl]-2-(4S-methoxyphenyl)-3R-pyrrolidinecarboxylic acid, monohydrochloride
CAS Number
195733-43-8
Synonyms
  • A-127722
  • A-147627
  • ABT-627
Molecular Formula
C29H38N2O6 • HCl
Formula Weight
547.1
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Soluble: ≥10 mg/ml
SMILES
O=C(N(CCCC)CCCC)CN1[C@](C2=CC=C(OC)C=C2)([H])[C@H](C(O)=O)[C@](C3=CC=C(OCO4)C4=C3)([H])C1.Cl
InChi Code
InChI=1S/C29H38N2O6.ClH/c1-4-6-14-30(15-7-5-2)26(32)18-31-17-23(21-10-13-24-25(16-21)37-19-36-24)27(29(33)34)28(31)20-8-11-22(35-3)12-9-20;/h8-13,16,23,27-28H,4-7,14-15,17-19H2,1-3H3,(H,33,34);1H/t23-,27-,28+;/m1./s1
InChi Key
IJFUJIFSUKPWCZ-SQMFDTLJSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    25 mg

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    Product Description

    Atrasentan is an antagonist of endothelin receptor type A (ETA; Ki = 69 pM for the human receptor).1 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.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Opgenorth, T.J., Adler, A.L., Calzadilla, S.V., et al. Pharmacological characterization of A-127722: An orally active and highly potent ETA-selective receptor antagonist. J. Pharmacol. Exp. Ther. 276(2), 473-481 (1996).

    2. Sasser, J.M., Sullivan, J.C., Hobbs, J.L., et al. Endothelin A receptor blockade reduces diabetic renal injury via an anti-inflammatory mechanism. J. Am. Soc. Nephrol. 18(1), 143-154 (2007).