A potent ETA receptor antagonist
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Sitaxentan (sodium salt)

Item No. 29244

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(4-chloro-3-methyl-5-isoxazolyl)-2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]-3-thiophenesulfonamide, monosodium salt
CAS Number
210421-74-2
Synonyms
  • TBC 11251
  • Thelin
Molecular Formula
C18H14ClN2O6S2 • Na
Formula Weight
476.9
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 10mg/mLDMSO: 15mg/mLDMSO:PBS (pH 7.2) (1:6): 0.14mg/mLEthanol: 5mg/mL
λmax
266 nm
SMILES
CC1=C(CC(C2=C(S([N-]C3=C(Cl)C(C)=NO3)(=O)=O)C=CS2)=O)C=C4C(OCO4)=C1.[Na+]
InChi Code
InChI=1S/C18H14ClN2O6S2.Na/c1-9-5-13-14(26-8-25-13)7-11(9)6-12(22)17-15(3-4-28-17)29(23,24)21-18-16(19)10(2)20-27-18;/h3-5,7H,6,8H2,1-2H3;/q-1;+1
InChi Key
MDTNUYUCUYPIHE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

    $50

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    10 mg

    $95

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    25 mg

    $174

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    Product Description

    Sitaxentan is a potent nonpeptide endothelin A (ETA) receptor antagonist (IC50 = 1.4 nM).1 It is selective for ETA over ETB receptors (IC50 = 9,800 nM). Sitaxentan inhibits phosphoinositol hydrolysis induced by endothelin-1 (Item No. 24127) in COS-7 cells (pA2 = 8). In vivo, sitaxentan reduces blood pressure in a rat model of acute hypoxia-induced pulmonary hypertension (ED50 = 0.5 mg/kg). It reduces femoral artery neointimal lesion size in a mouse model of intraluminal injury.2 Sitaxentan (15 mg/kg) decreases bronchoalveolar lavage fluid (BALF) pleocytosis, as well as pulmonary collagen deposition and fibrosis, and improves lung mechanics in a mouse model of bleomycin-induced lung injury.3 Formulations containing sitaxentan have been used in the treatment of hypertension.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wu, C., Chan, M.F., Stavros, F.L., et al. Discovery of TBC11251, a potent, long acting, orally active endothelin receptor-A selective antagonist. J. Med. Chem. 40(11), 1690-1697 (1997).

    2. Duthie, K.M., Hadoke, P.W., Kirkby, N.S., et al. Selective endothelin A receptor antagonism with sitaxentan reduces neointimal lesion size in a mouse model of intraluminal injury. Br. J. Pharmacol. 172(11), 2827-2837 (2015).

    3. Manitsopoulos, N., Nikitopoulos, I., Maniatis, N.A., et al. Highly selective endothelin-1 receptor A inhibition prevents bleomycin-induced pulmonary inflammation and fibrosis in mice. Respiration 95(2), 122-136 (2018).