An ETA receptor antagonist
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Clazosentan

Item No. 46195

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-[2-(2H-tetrazol-5-yl)-4-pyridinyl]-4-pyrimidinyl]-5-methyl-2-pyridinesulfonamide
CAS Number
180384-56-9
Synonyms
  • AXV-034343
  • Ro 61-1790
  • VML 588
Molecular Formula
C25H23N9O6S
Formula Weight
577.6
Purity
≥98%
Formulation (Request formulation change)
A solid
SMILES
O=S(NC1=NC(C2=CC=NC(C3=NN=NN3)=C2)=NC(OCCO)=C1OC4=C(C=CC=C4)OC)(C5=NC=C(C)C=C5)=O
InChi Code
InChI=1S/C25H23N9O6S/c1-15-7-8-20(27-14-15)41(36,37)32-24-21(40-19-6-4-3-5-18(19)38-2)25(39-12-11-35)29-22(28-24)16-9-10-26-17(13-16)23-30-33-34-31-23/h3-10,13-14,35H,11-12H2,1-2H3,(H,28,29,32)(H,30,31,33,34)
InChi Key
LFWCJABOXHSRGC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $48

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    5 mg

    $216

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    10 mg

    $336

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    25 mg

    $540

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    Product Description

    Clazosentan is an endothelin type A (ETA) receptor antagonist.1 It selectively inhibits ET-1-stimulated calcium mobilization in HEK293 cells expressing the ETA over the ETB receptor (IC50s = 0.23 and 422 nM, respectively). When administered intravenously, clazosentan inhibits the ET-1-induced pressor response in anesthetized, pithed rats and reverses cerebral vasospasm in a dog model of subarachnoid hemorrhage (SAH).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Roux, S., Breu, V., Giller, T., et al. Ro 61-1790, a new hydrosoluble endothelin antagonist: General pharmacology and effects on experimental cerebral vasospasm. J. Pharmacol. Exp. Ther. 283(3), 1110-1118 (1997).