Darusentan

For research use only, not for therapeutic use.

  • CAT Number: M128036
  • CAS Number: 171714-84-4
  • Molecular Formula: C22H22N2O6
  • Molecular Weight: 410.426
  • Purity: ≥95%
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Darusentan, also known as Lu 135252 and HMR-4005, is anEndothelin-1 receptor A inhibitor for the potential treatment of uncontrolled hypertension and cancer. Darusentan is a potent inhibitor of endothelin signaling and function in both large and small arteries. Endothelin ETA receptor blockade with darusentan increases sodium and potassium excretion in aging rats.


Catalog Number M128036
CAS Number 171714-84-4
Molecular Formula C22H22N2O6
Purity ≥95%
Storage -20°C
IUPAC Name (2S)-2-(4,6-dimethoxypyrimidin-2-yl)oxy-3-methoxy-3,3-diphenylpropanoic acid
InChI InChI=1S/C22H22N2O6/c1-27-17-14-18(28-2)24-21(23-17)30-19(20(25)26)22(29-3,15-10-6-4-7-11-15)16-12-8-5-9-13-16/h4-14,19H,1-3H3,(H,25,26)/t19-/m1/s1
InChIKey FEJVSJIALLTFRP-LJQANCHMSA-N
SMILES COC1=CC(=NC(=N1)OC(C(=O)O)C(C2=CC=CC=C2)(C3=CC=CC=C3)OC)OC
Reference

</br>1:Endothelin-1 receptor A blocker darusentan decreases hepatic changes and improves liver repopulation after cell transplantation in rats. Bahde R, Kapoor S, Viswanathan P, Spiegel HU, Gupta S.Hepatology. 2014 Mar;59(3):1107-17. doi: 10.1002/hep.26766. Epub 2014 Jan 16. PMID: 24114775 Free PMC Article</br>2:Physiology of endothelin in producing myocardial perfusion heterogeneity: a mechanistic study using darusentan and positron emission tomography. Johnson NP, Gould KL.J Nucl Cardiol. 2013 Oct;20(5):835-44. doi: 10.1007/s12350-013-9756-5. Epub 2013 Jul 11. PMID: 23842710 Free PMC Article</br>3:Determination of darusentan enantiomers in rat plasma by enantioselective liquid chromatography with tandem mass spectrometry using cellulose-based chiral stationary phase. Gu J, Shi X, Du Y, Wang W, Du X, Zhang L.J Sep Sci. 2011 Oct;34(19):2680-5. doi: 10.1002/jssc.201100433. Epub 2011 Aug 8. PMID: 21823235 </br>4:Divergent results using clinic and ambulatory blood pressures: report of a darusentan-resistant hypertension trial. Bakris GL, Lindholm LH, Black HR, Krum H, Linas S, Linseman JV, Arterburn S, Sager P, Weber M.Hypertension. 2010 Nov;56(5):824-30. doi: 10.1161/HYPERTENSIONAHA.110.156976. Epub 2010 Oct 4. PMID: 20921430 Free Article</br>5:Darusentan is a potent inhibitor of endothelin signaling and function in both large and small arteries. Liang F, Glascock CB, Schafer DL, Sandoval J, Cable L, Melvin L Jr, Hartman JC, Pitts KR.Can J Physiol Pharmacol. 2010 Aug;88(8):840-9. doi: 10.1139/Y10-061. PMID: 20725142 Free Article</br>6:Darusentan, a selective endothelin A receptor antagonist, for the oral treatment of resistant hypertension. Enseleit F, Lüscher TF, Ruschitzka F.Ther Adv Cardiovasc Dis. 2010 Aug;4(4):231-40. doi: 10.1177/1753944710373785. Epub 2010 Jul 26. Review. PMID: 20660536 </br>7:Evaluation of the endothelin receptor antagonists ambrisentan, darusentan, bosentan, and sitaxsentan as substrates and inhibitors of hepatobiliary transporters in sandwich-cultured human hepatocytes. Hartman JC, Brouwer K, Mandagere A, Melvin L, Gorczynski R.Can J Physiol Pharmacol. 2010 Jun;88(6):682-91. doi: 10.1139/Y10-060. PMID: 20628435 Free Article</br>8:Darusentan in resistant hypertension: lost in translation. Enseleit F, Ruschitzka F.Curr Hypertens Rep. 2010 Feb;12(1):1-3. doi: 10.1007/s11906-009-0081-y. No abstract available. PMID: 20425150 </br>9:Dietary alkalinization and darusentan for prevention of decline in glomerular filtration rate in rats fed a casein diet. Bakker SJ, Gans RO, Navis G.Kidney Int. 2008 Dec;74(12):1625-6; author reply 1626-7. doi: 10.1038/ki.2008.434. No abstract available. PMID: 19034308 Free Article</br>10:Darusentan: a new perspective for treatment of resistant hypertension? Enseleit F, Lüscher TF, Ruschitzka F.Expert Opin Investig Drugs. 2008 Aug;17(8):1255-63. doi: 10.1517/13543784.17.8.1255 . Review. PMID: 18616421

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