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PF-3274167

Oral oxytocin antagonist CAS# 900510-03-4

PF-3274167

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Chemical structure

PF-3274167

3D structure

Chemical Properties of PF-3274167

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.
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.
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.

Biological Activity of PF-3274167

DescriptionPF-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:
[1]. 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):2547-2552. [2]. Brown A, et al. Triazole oxytocin antagonists: Identification of an aryloxyazetidine replacement for a biaryl substituent. Bioorg Med Chem Lett. 2010 Jan 15;20(2):516-520.

PF-3274167 Dilution Calculator

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PF-3274167 Molarity Calculator

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Preparing Stock Solutions of PF-3274167

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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Background on PF-3274167

PF-3274167 is an oral oxytocin antagonist.

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References on PF-3274167

[(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.

Description

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.

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