Cligosiban

Cligosiban (PF-3274167) is an orally active, highly selective, and centrally permeable oxytocin receptor antagonist with good pharmacokinetics in rats and can inhibit physiological ejaculation in rodents[1][2].

Product Specifications

CAS Number

[900510-03-4]

Product Name Alternative

PF-3274167

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Oxytocin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Field of Research

Endocrinology

Assay Protocol

https://www.medchemexpress.com/PF-3274167.html

Purity

99.95

Solubility

DMSO : ≥ 50 mg/mL

Smiles

FC1=CC(Cl)=C(OC2CN(C3=NN=C(COC)N3C4=CC=C(OC)N=C4)C2)C=C1

Molecular Formula

C19H19ClFN5O3

Molecular Weight

419.84

Precautions

H302, H315, H319, H335

References & Citations

[1]Wayman C, et al. Cligosiban, A Novel Brain-Penetrant, Selective Oxytocin Receptor Antagonist, Inhibits Ejaculatory Physiology in Rodents. J Sex Med. 2018 Dec;15 (12) :1698-1706. |[2]Yue X, et al. Pharmacokinetics, bioavailability and metabolism of cligosiban, an antagonist of oxytocin receptor, in rat by liquid chromatography hyphenated with electrospray ionization tandem mass spectrometry. J Pharm Biomed Anal. 2019 Feb 5;164:725-733. |[3]Badshah M, et al. The Effects of Age on Prostatic Responses to Oxytocin and the Effects of Antagonists. Biomedicines. 2023 Nov 1;11 (11) :2956. |[4]Badshah M, et al. Age-Dependent Effects of Oxytocin and Oxytocin Receptor Antagonists on Bladder Contractions: Implications for the Treatment of Overactive Bladder Syndrome. Biomedicines. 2024 Mar 18;12 (3) :674.