An ETA and ETB antagonist
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Ro 46-2005

Item No. 43523

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(1,1-dimethylethyl)-N-[6-(2-hydroxyethoxy)-5-(3-methoxyphenoxy)-4-pyrimidinyl]-benzenesulfonamide
CAS Number
150725-87-4
Molecular Formula
C23H27N3O6S
Formula Weight
473.5
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/ml
SMILES
CC(C)(C1=CC=C(S(NC2=C(C(OCCO)=NC=N2)OC3=CC=CC(OC)=C3)(=O)=O)C=C1)C
InChi Code
InChI=1S/C23H27N3O6S/c1-23(2,3)16-8-10-19(11-9-16)33(28,29)26-21-20(22(25-15-24-21)31-13-12-27)32-18-7-5-6-17(14-18)30-4/h5-11,14-15,27H,12-13H2,1-4H3,(H,24,25,26)
InChi Key
ZNXOKLWCOWOECF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $64

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    10 mg

    $77

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    25 mg

    $160

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    Product Description

    Ro 46-2005 is an antagonist of endothelin receptor type A (ETA) and ETB (IC50s = 220 and 160 nM, respectively).1 It inhibits endothelin-1-induced secretion of arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607) in primary rat mesangial cells (IC50 = 1.8 µM). Ro 46-2005 prevents sarafotoxin S6-induced relaxation in preconstricted rat mesenteric arteries (pA2 = 6.47).2 It increases cerebral blood flow in a rat model of subarachnoid hemorrhage when administered at a dose of 3 mg/kg. Ro 46-2005 (30 or 100 mg/kg) decreases systolic blood pressure in sodium-depleted monkeys.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Breu, V., Löffler, B.-M., and Clozel, M. In vitro characterization of Ro 46-2005, a novel synthetic non-peptide endothelin antagonist of ETA and ETB receptors. FEBS Lett. 334(2), 210-214 (1993).

    2. Clozel, M., Breu, V., Burri, K., et al. Pathophysiological role of endothelin revealed by the first orally active endothelin receptor antagonist. Nature 365(6448), 759-761 (1993).