An ETA receptor antagonist
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Darusentan

Item No. 36034

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
αS-[(4,6-dimethoxy-2-pyrimidinyl)oxy]-β-methoxy-β-phenyl-benzenepropanoic acid
CAS Number
171714-84-4
Synonyms
  • HMR 4005
  • Lu 135252
Molecular Formula
C22H22N2O6
Formula Weight
410.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 2 mg/mlEthanol: 2 mg/mlPBS (pH 7.2): insol
SMILES
COC1=NC(O[C@H](C(O)=O)C(C2=CC=CC=C2)(C3=CC=CC=C3)OC)=NC(OC)=C1
InChi Code
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
InChi Key
FEJVSJIALLTFRP-LJQANCHMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $39

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    5 mg

    $136

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    10 mg

    $231

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    25 mg

    $530

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    Product Description

    Darusentan is an endothelin type A (ETA) receptor antagonist (Ki = 13 nM in rat aortic vascular smooth muscle cells).1 It inhibits contractions induced by human endothelin-1 (ET-1; Item No. 24127) in isolated rat aortic rings and mesenteric microvessels with pA2 values of 8.1 and 7.97, respectively. Darusentan (50 mg/kg) decreases systolic blood pressure in DOCA-salt hypertensive rats, as well as reduces mean arterial pressure (MAP) and left ventricular developed pressure (LVDP) in normotensive pigs when administered at doses of 1 and 5 mg/kg.2,3 It reduces myocardial infarct size as a percentage of the area at risk in a porcine model of ischemia-reperfusion injury induced by ligation of the left anterior descending (LAD) coronary artery.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Liang, F., Glascock, C.B., Schafer, D.L., et al. Darusentan is a potent inhibitor of endothelin signaling and function in both large and small arteries. Can. J. Physiol. Pharmacol. 88(8), 840-849 (2010).

    2. Schiffrin, E.L., Turgeon, A., and Deng, L.Y. Effect of chronic ETA-selective endothelin receptor antagonism on blood pressure in experimental and genetic hypertension in rats. Br. J. Pharmacol. 121(5), 935-940 (1997).

    3. Gonon, A.T., Wang, Q.D., Shimizu, M., et al. The novel non-peptide selective endothelin A receptor antagonist LU 135 252 protects against myocardial ischaemic and reperfusion injury in the pig. Acta Physiol. Scand. 163(2), 131-137 (1998).