Free shipping starts now, no minimum, no coupons required!

Darusentan

LU 135252

A Selective Antagonist of Endothelin A Receptors

Cat #: D-265
Alternative Name LU 135252
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 410.43
    Purity: >99%
    Effective concentration 1 nM – 1 µM.
    Structure
    Chemical name (2S)-2-(4,6-dimethoxypyrimidin-2-yl)oxy-3-methoxy-3,3-diphenylpropanoic acid.
    Molecular formula C22H22N2O6.
    CAS No.: 171714-84-4
    PubChem CID 177236
    Activity Darusentan is a selective antagonist of ET-A Endothelin receptors, inhibiting Endothelin-1 radioligand binding to ET-A and ET-B receptors with Ki of 6 nM and 371 nM, respectively1in vitro Darusentan inhibits Endothelin-induced vascular contractility in isolated endothelium-denuded rat aortic rings with pA2 of 8.12. Darusentan is orally bioavailable and active in vivo3.
    References-Activity
    1. Riechers, H. et al. (1996) J. Med. Chem. 39, 2123.
    2. Liang, F. et al. (2010) Can. J. Physiol. Pharmacol. 88, 840.
    3. Prié, S. et al. (1997) J. Pharmacol. Exp. Ther.  282, 1312.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
    Storage of solutions Up to three months at -20°C.
    Our bioassay
    • Alomone Labs Darusentan inhibits ET-A receptor-mediated Ca2+ mobilization in CHO-K1 cells.
      Alomone Labs Darusentan inhibits ET-A receptor-mediated Ca2+ mobilization in CHO-K1 cells.
      Dose response curve of Darusentan (#D-265) inhibition of ET-A receptor-mediated, Endothelin-1-evoked Ca2+ mobilization. IC50 was determined at 10.96 nM.
      Cells were loaded with Calcium 6 dye, incubated with Darusentan, and stimulated with 15 nM Endothelin-1 (EC80). Changes in intracellular Ca2+ levels were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™.
    References - Scientific background
    1. Liang, F. et al. (2010) Can. J. Physiol. Pharmacol. 88, 840.
    2. Enseleit, F. et al. (2010) Ther. Adv. Cardiovasc. Dis. 4, 231.
    3. Saeki, T. et al. (1991) Biochem. Biophys. Res. Commun. 179, 286.
    Scientific background

    Darusentan, (LU 135252), is a synthetic compound that acts as a selective antagonist of endothelin A (ET-A) receptors. Darusentan is orally bioavailable and is a potent inhibitor of vasoconstriction in large and small arteries. The compound is a propanoic acid based antagonist that consist of two enantiomers - (R) and (S). The (R) enantiomer shows no binding activity, indicating that the (S) enantiomer is the active drug1,2.

    in vitro, Darusentan inhibits endothelin-induced vascular contractility in isolated endothelium-denuded rat aortic rings with pA2 value of 8.11,2.

    Endothelin receptors include two subtypes: ET-A and ET-B. They are widely distributed in vascular and nonvascular tissues. ET-A receptors are predominantly expressed in peripheral tissues, especially in vascular smooth muscle tissues to mediate vasoconstriction. They are also detected in several different regions of the brain3.

    Target ET-A receptors
    Last update: 06/11/2022

    Darusentan (#D-265) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
    Shipping and Ordering information