A vasopressin receptor V1a antagonist
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SR 49059

Item No. 17972

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[[(2R,3S)-5-chloro-3-(2-chlorophenyl)-1-[(3,4-dimethoxyphenyl)sulfonyl]-2,3-dihydro-3-hydroxy-1H-indol-2-yl]carbonyl]-2-pyrrolidinecarboxamide
CAS Number
150375-75-0
Synonyms
  • Relcovaptan
Molecular Formula
C28H27Cl2N3O7S
Formula Weight
620.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMSO: 5 mg/mlEthanol: 5 mg/ml
SMILES
ClC1=CC=CC=C1[C@]2(O)[C@H](C(N3CCC[C@H]3C(N)=O)=O)N(S(C4=CC=C(OC)C(OC)=C4)(=O)=O)C5=CC=C(Cl)C=C52
InChi Code
InChI=1S/C28H27Cl2N3O7S/c1-39-23-12-10-17(15-24(23)40-2)41(37,38)33-21-11-9-16(29)14-19(21)28(36,18-6-3-4-7-20(18)30)25(33)27(35)32-13-5-8-22(32)26(31)34/h3-4,6-7,9-12,14-15,22,25,36H,5,8,13H2,1-2H3,(H2,31,34)/t22-,25-,28+/m0/s1
InChi Key
CEBYCSRFKCEUSW-NAYZPBBASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $54

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    5 mg

    $185

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    10 mg

    $341

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    25 mg

    $717

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    Product Description

    SR 49059 is a selective, nonpeptide antagonist of the V1a subtype of the vasopressin receptor (Ki = 1.1-6.3 nM in human).1,2 It demonstrates ≥2 orders of magnitude lower affinity for V1b, V2, and oxytocin receptors and does not exhibit any intrinsic agonist activity.1 SR 49059 can inhibit arginine vasopressin-induced human platelet aggregation with an IC50 value of 3.7 nM.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Serradiel-Le Gal, C., Wagnon, J., Garcia, C., et al. Biochemical and pharmacological properties of SR 49059, a new, potent, nonpeptide antagonist of rat and human vasopressin V1a receptors. J. Clin. Invest. 92(1), 224-231 (1993).

    2. Thibonnier, M., Conarty, D.M., Preston, J.A., et al. Molecular pharmacology of human vasopressin receptors. Vasopressin and Oxytocin 1, 251-276 (1998).