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PF3274167

Name: PF3274167
Brand: TargetMol
SKU: T3347
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T3347Cas No. 900510-03-4

Alias PF-3274167, PF 3274167, Cligosiban

PF3274167 (Cligosiban) is a potent and selective, high-affinity nonpeptide oxytocin receptor antagonist.

PF3274167

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Purity: 99.88%

Catalog No. T3347Alias PF-3274167, PF 3274167, CligosibanCas No. 900510-03-4

PF3274167 (Cligosiban) is a potent and selective, high-affinity nonpeptide oxytocin receptor antagonist.

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$30	In Stock	In Stock
10 mg	$46	In Stock	In Stock
25 mg	$95	In Stock	In Stock
50 mg	$153	In Stock	In Stock
100 mg	$247	-	In Stock
1 mL x 10 mM (in DMSO)	$31	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.88%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

PF3274167 AI Summary

PF3274167 exhibits a range of bioactivities and pharmacokinetic properties. Primarily, it demonstrates antagonist activity at the human oxytocin receptor (OTR) with a Ki of 9.5 nM and at the vasopressin V1a receptor with a Ki of 1120.0 nM, showing low activity at the vasopressin V2 receptor (Ki > 10000.0 nM). The compound also binds to the NK1 receptor (Ki = 6500.0 nM), kappa opioid receptor (Ki = 3000.0 nM), and ghrelin receptor (Ki = 4400.0 nM). It displays moderate oral bioavailability in rats (62.0%) and dogs (81.0%), with notable intrinsic clearance in human liver microsomes (10.0 ug/min/mg). In terms of antiviral properties, PF3274167 inhibits SARS-CoV-2 induced cytotoxicity in Caco-2 and VERO-6 cells, though with varying percentages of inhibition. Additionally, it has shown inhibitory activity against the SARS-CoV-2 3CL-Pro protease and human HDAC6 enzymes. The half-life, unbound fraction in plasma and brain, and other pharmacokinetic parameters further highlight its potential therapeutic applications across different species..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	PF3274167 (Cligosiban) is a potent and selective, high-affinity nonpeptide oxytocin receptor antagonist.
Targets&IC50	OTR:9.5 nM
Synonyms	PF-3274167, PF 3274167, Cligosiban

Chemical Properties

Molecular Weight	419.84
Formula	C₁₉H₁₉ClFN₅O₃
Cas No.	900510-03-4
Smiles	C(OC)C=1N(C(=NN1)N2CC(OC3=C(Cl)C=C(F)C=C3)C2)C=4C=CC(OC)=NC4
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 55 mg/mL (131 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2.5 mg/mL (5.95 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3819 mL	11.9093 mL	23.8186 mL	119.0930 mL
5 mM	0.4764 mL	2.3819 mL	4.7637 mL	23.8186 mL
10 mM	0.2382 mL	1.1909 mL	2.3819 mL	11.9093 mL
20 mM	0.1191 mL	0.5955 mL	1.1909 mL	5.9546 mL
50 mM	0.0476 mL	0.2382 mL	0.4764 mL	2.3819 mL
100 mM	0.0238 mL	0.1191 mL	0.2382 mL	1.1909 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc