PF-3274167 manufacturers
- PF3274167
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- $30.00
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2026-07-13
- CAS:900510-03-4
- Purity: 99.88%
- Supply Ability: 10g
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| | PF-3274167 Basic information |
| Product Name: | PF-3274167 | | Synonyms: | PF-3274167;PF-03274167;5-[3-[3-(2-Chloro-4-fluorophenoxy)-1-azetidinyl]-5-(methoxymethyl)-4H-1,2,4-triazol-4-yl]-2-methoxypyridine;5-[3-[3-(2-chloro-4-fluorophenoxy)azetidin-1-yl]-5-(methoxymethyl)-1,2,4-triazol-4-yl]-2-methoxypyridine;Cligosiban;PF 3274167;PF3274167;PF-3274167(cligosiban);5-(3-(3-(2-Chloro-4-fluorophenoxy)azetidin-1-yl)-5-(methoxymethyl)-4H-1,2,4-triazol-4-yl)-2-methoxypyridine | | CAS: | 900510-03-4 | | MF: | C19H19ClFN5O3 | | MW: | 419.84 | | EINECS: | | | Product Categories: | | | Mol File: | 900510-03-4.mol |  |
| | PF-3274167 Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO: 18 mg/mL | | form | A crystalline solid | | color | Off-white to pink |
| | PF-3274167 Usage And Synthesis |
| Description | PF-3274167 is an oxytocin receptor antagonist (Ki = 9.5 nM). It is selective for the oxytocin receptor over the vasopressin receptors V1A and V2 (Kis = 1,120 and 10,000 nM, respectively). | | Uses | PF-3274167 functions as s triazole oxytocin antagonists. It also functions as a PET radiotracer of oxytocin receptors. | | in vivo | Cligosiban (0.9 mg/kg; 3 to 5 minutes after injection of Apomorphine (HY-12723); i.v.) shows CNS permeability and inhibits Apomorphine-induced ejaculation in an anesthetized rat CNS neuronal discharge model by modulating oxytocin (OT)-mediated responses in the nucleus tractus solitarius (NTS)[1].
Cligosiban (1 mg/kg; i.v. or p.o.) produces 4 metabolites in rat plasma, with demethylation and glucuronidation being the major metabolic pathways, and the pharmacokinetic profile is favorable[2]. | Animal Model: | Male Sprague Dawley rats (280-350 g), Anesthetized Rat CNS Neuronal Firing Model (Pre injection of Apomorphine (200 mg/kg, intravenous injection) into rats to regulate neuronal firing)[1]. | | Dosage: | 0.9 mg/kg | | Administration: | Intravenous injection (i.v.); 3 to 5 minutes after injection of Apomorphine | | Result: | Reversed the reduced firing of nucleus tractus solitaries (NTS) neurons induced by Apomorphine and reduced the bulbospongiosum burst pattern and contraction amplitude associated with ejaculation. |
| Animal Model: | Male Sprague-Dawley rats with body weight of 200-220g[2]. | | Dosage: | 1 mg/kg | | Administration: | Intravenous injection (i.v.) or oral gavage (p.o.) | | Result: | Was rapidly absorbed into the plasma after oral administration and reached its maximum blood concentration 1.41 hours after administration, and was quickly eliminated from the plasma after absorption. |
| | References | [1] ALAN BROWN. Triazole oxytocin antagonists: Identification of an aryloxyazetidine replacement for a biaryl substituent[J]. Bioorganic & Medicinal Chemistry Letters, 2010, 20 2: Pages 516-520. DOI: 10.1016/j.bmcl.2009.11.097 |
| | PF-3274167 Preparation Products And Raw materials |
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