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PF-3274167
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
PF-3274167图片
CAS NO:900510-03-4
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Oral oxytocin antagonist
Cas No.900510-03-4
化学名5-(3-(3-(2-chloro-4-fluorophenoxy)azetidin-1-yl)-5-(methoxymethyl)-4H-1,2,4-triazol-4-yl)-2-methoxypyridine
Canonical SMILESCOCC(N1C2=CN=C(OC)C=C2)=NN=C1N3CC(OC4=C(Cl)C=C(F)C=C4)C3
分子式C19H19ClFN5O3
分子量419.84
溶解度≥ 18.15mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Cligosiban (PF-3274167), a high oral bioavailability and good brain-penetrant non-peptide oxytocin receptor antagonist, shows a high-affinity (Ki=9.5 nM) and an excellent selectivity versus the vasopressin receptors with almost no affinity for the V1b and V1a subtypes. Cligosiban inhibits ejaculatory physiology in rodents[1][2].

References:
[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]. Karpenko IA, et al. Selective nonpeptidic fluorescent ligands for oxytocin receptor: design, synthesis, and application to time-resolved FRET binding assay. J Med Chem. 2015 Mar 12;58(5):2547-52.