Date published: 2026-5-17

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SR 49059 (CAS 150375-75-0)

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Alternate Names:
Relcovaptan
Application:
SR 49059 is a potent and selective AVP Receptor V1a antagonist
CAS Number:
150375-75-0
Purity:
≥99%
Molecular Weight:
620.50
Molecular Formula:
C28H27Cl2N3O7S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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SR 49059 is a potent and selective antagonist of neurokinin-1 (NK1) receptors. It functions by binding to the NK1 receptor and blocking the binding of substance P, a neuropeptide involved in pain transmission and inflammation. By inhibiting the action of substance P at the molecular level, SR 49059 effectively disrupts the signaling pathway mediated by NK1 receptors. This interference ultimately leads to the suppression of neurogenic inflammation and pain perception. In experimental applications, SR 49059 is utilized to investigate the role of NK1 receptors in various physiological and pathological processes, particularly those related to pain and inflammation. Its mechanism of action involves targeting and inhibiting the activity of NK1 receptors, shedding light on the mechanisms underlying pain transmission and inflammatory responses.


SR 49059 (CAS 150375-75-0) References

  1. Evidence for an involvement of vasopressin in mechanism of primary dysmenorrhea and effect of the non-peptide vasopressin V1a receptor antagonist, SR 49059, on the uterus of non-pregnant women.  |  Akerlund, M., et al. 1998. Adv Exp Med Biol. 449: 467-72. PMID: 10026840
  2. Receptor binding of oxytocin and vasopressin antagonists and inhibitory effects on isolated myometrium from preterm and term pregnant women.  |  Akerlund, M., et al. 1999. Br J Obstet Gynaecol. 106: 1047-53. PMID: 10519430
  3. A nonpeptide vasopressin V(1a) receptor antagonist, SR 49059, does not prevent cisplatin-induced emesis in piglets.  |  Grélot, L., et al. 2001. Fundam Clin Pharmacol. 15: 189-200. PMID: 11468030
  4. Effects of nonpeptide V(1) vasopressin receptor antagonist SR-49059 on infarction volume and recovery of function in a focal embolic stroke model.  |  Shuaib, A., et al. 2002. Stroke. 33: 3033-7. PMID: 12468809
  5. Central effect of vasotocin 4 receptor (VT4R/V1aR) antagonists on the stress response and food intake in chicks given neuropeptide Y (NPY).  |  Kuenzel, WJ., et al. 2016. Neurosci Lett. 620: 57-61. PMID: 27016389
  6. Effect of SR-49059, a vasopressin V1a antagonist, on human vascular smooth muscle cells.  |  Serradeil-Le Gal, C., et al. 1995. Am J Physiol. 268: H404-10. PMID: 7840290
  7. Binding of [3H] SR 49059, a potent nonpeptide vasopressin V1a antagonist, to rat and human liver membranes.  |  Serradeil-Le Gal, C., et al. 1994. Biochem Biophys Res Commun. 199: 353-60. PMID: 8123034
  8. Effect of a new, potent, non-peptide V1a vasopressin antagonist, SR 49059, on the binding and the mitogenic activity of vasopressin on Swiss 3T3 cells.  |  Serradeil-Le Gal, C., et al. 1994. Biochem Pharmacol. 47: 633-41. PMID: 8129742
  9. Biochemical and pharmacological properties of SR 49059, a new, potent, nonpeptide antagonist of rat and human vasopressin V1a receptors.  |  Serradeil-Le Gal, C., et al. 1993. J Clin Invest. 92: 224-31. PMID: 8392086
  10. Potent inhibitory effect of SR 49059, an orally active non-peptide vasopressin VIa receptor antagonist, on human arterial coronary bypass graft.  |  Liu, JJ., et al. 1995. Clin Sci (Lond). 89: 481-5. PMID: 8549062
  11. Effect of the non-peptide, vasopressin V1a receptor antagonist, SR 49059 and its enantiomer, SR 49770, on isolated human myometrium.  |  Bossmar, T., et al. 1996. Acta Obstet Gynecol Scand. 75: 516-9. PMID: 8693925
  12. Determination of SR 49059 in human plasma and urine by LC-APCI/MS/MS.  |  Burton, R., et al. 1997. J Pharm Biomed Anal. 15: 1913-22. PMID: 9278897
  13. Effects of the vasopressin V1a receptor antagonist, SR 49059, on the response of human uterine arteries to vasopressin and other vasoactive substances.  |  Kostrzewska, A., et al. 1998. Acta Obstet Gynecol Scand. 77: 3-7. PMID: 9492709

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

SR 49059, 10 mg

sc-204300
10 mg
$354.00