PF-3274167Oral oxytocin antagonist CAS# 900510-03-4 |
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Quality Control & MSDS
3D structure
Package In Stock
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| Cas No. | 900510-03-4 | SDF | Download SDF |
| PubChem ID | 11683187 | Appearance | Powder |
| Formula | C19H19ClFN5O3 | M.Wt | 419.84 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | cligosiban | ||
| Solubility | DMSO : ≥ 50 mg/mL (119.09 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 5-[3-[3-(2-chloro-4-fluorophenoxy)azetidin-1-yl]-5-(methoxymethyl)-1,2,4-triazol-4-yl]-2-methoxypyridine | ||
| SMILES | COCC1=NN=C(N1C2=CN=C(C=C2)OC)N3CC(C3)OC4=C(C=C(C=C4)F)Cl | ||
| Standard InChIKey | HNIFCPBQMKPRCX-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C19H19ClFN5O3/c1-27-11-17-23-24-19(26(17)13-4-6-18(28-2)22-8-13)25-9-14(10-25)29-16-5-3-12(21)7-15(16)20/h3-8,14H,9-11H2,1-2H3 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | PF-3274167 is a high-affinity nonpeptide oxytocin receptor (OTR) antagonist, with Ki of 9.5 nM.
IC50 value: 9.5 nM [1]
Target: oxytocin receptor (OTR) References: | |||||
PF-3274167 Dilution Calculator
PF-3274167 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.3819 mL | 11.9093 mL | 23.8186 mL | 47.6372 mL | 59.5465 mL |
| 5 mM | 0.4764 mL | 2.3819 mL | 4.7637 mL | 9.5274 mL | 11.9093 mL |
| 10 mM | 0.2382 mL | 1.1909 mL | 2.3819 mL | 4.7637 mL | 5.9546 mL |
| 50 mM | 0.0476 mL | 0.2382 mL | 0.4764 mL | 0.9527 mL | 1.1909 mL |
| 100 mM | 0.0238 mL | 0.1191 mL | 0.2382 mL | 0.4764 mL | 0.5955 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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PF-3274167 is an oral oxytocin antagonist.
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[(11)C]PF-3274167 as a PET radiotracer of oxytocin receptors: Radiosynthesis and evaluation in rat brain.[Pubmed:28917111]
Nucl Med Biol. 2017 Dec;55:1-6.
INTRODUCTION: Oxytocin plays a major role in the regulation of social interactions in mammals by interacting with the oxytocin receptor (OTR) expressed in the brain. Furthermore, the oxytocin system appears as a possible therapeutic target in autism spectrum disorders and other psychiatric troubles, justifying current pharmacological researches. Since no specific PET radioligand is currently available to image OTR in the brain, the aim of this study was to radiolabel the specific OTR antagonist PF-3274167 and to evaluate [(11)C]PF-3274167 as a potential PET tracer for OTR in rat brains. METHODS: [(11)C]PF-3274167 was prepared via the O-methylation of its desmethyl precursor with [(11)C]methyl iodide. The lipophilicity of the radioactive compound was evaluated by measuring the n-octanol-buffer partition coefficient (logD). Autoradiography experiments were performed on rat brain tissue to evaluate the in vitro distribution of the [(11)C]PF-3274167. MicroPET experiments were conducted with and without pre-injection of ciclosporin in order to evaluate the influence of the P-glycoprotein (P-gp) on the brain uptake. RESULTS: [(11)C]PF-3274167 was synthesized with high radiochemical and chemical purities (>95%) and good specific activity. The measured logD was 1.93. In vitro, [(11)C]PF-3274167 did not show any evidence of specific binding to OTR. PET imaging showed that [(11)C]PF-3274167 uptake in rat brain was very low in basal conditions but increased significantly after the administration of ciclosporin, suggesting that it is a substrate of the P-gp. In the ciclosporin-pre-injected rat, however, [(11)C]PF-3274167 distribution did not match with the known distribution of OTR in rats. CONCLUSION: [(11)C]PF-3274167 is not a suitable tracer for imaging of OTR in rat brain, probably because of a too low affinity for this receptor in addition to a poor brain penetration.
