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PF-06291874

Name: PF-06291874
Brand: TargetMol
SKU: TQ0239
Price: 80 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. TQ0239Cas No. 1393124-08-7

Alias Glucagon receptor antagonists-4

PF-06291874 (Glucagon receptor antagonists-4) (Glucagon receptor antagonists-4) is a highly effective and orally active antagonist of the glucagon receptor.

PF-06291874

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Purity: 99.27%

Catalog No. TQ0239Alias Glucagon receptor antagonists-4Cas No. 1393124-08-7

PF-06291874 (Glucagon receptor antagonists-4) (Glucagon receptor antagonists-4) is a highly effective and orally active antagonist of the glucagon receptor.

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$55	In Stock	In Stock
10 mg	$80	In Stock	In Stock
25 mg	Preferential	In Stock	In Stock
50 mg	Preferential	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$62	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:99.27%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

PF-06291874 AI Summary

PF-06291874 exhibits a diverse range of bioactivities, including significant permeability properties, receptor binding affinities, and varied inhibitory and modulatory effects across multiple cell types and receptors. It demonstrates apparent permeability across MDCK2 cells (Papp 3.6 ucm/s) and human Caco-2 cells (Papp 30.0 ucm/s at pH 6.5 and 8.5 ucm/s at pH 7.4), as well as across dog RRCK cells (8.5 x 10^-6 cm/s). It acts as an antagonist at various glucagon receptors in species including human, monkey, dog, mouse, and rats, with Kb values from 82.0 nM to 3900.0 nM, and displaces [125I]-glucagon-cex from the human glucagon receptor with a Ki value of 14.0 nM. The compound shows specific binding affinity to GLP-1 receptors (Ki 3160.0 nM) and inhibits the rat GABA-gated chloride channel (Ki 8200.0 nM). In terms of pharmacokinetics, PF-06291874 has 100% oral bioavailability in both Beagle dogs (5 mg/kg, half-life 2.5 hours, Vdss 0.31 L/kg) and Wistar-Han rats (50 mg/kg, half-life 1.8 hours, Vdss 0.4 L/kg). It also shows plasma clearance rates in Beagle dogs (1.5 mL/min/kg) and Wistar-Han rats (2.8 mL/min/kg). With a log D value of 2.5 at pH 7.4, the compound also demonstrates significant cytotoxicity against human THLE cells (IC50 112000.0 nM). Additionally, PF-06291874 shows cell type-dependent effects on cell viability, with varying growth rates in HEK293T, U2OS, and human fibroblast cells. Thermal Shift Assay results indicate that it has both stabilizing and destabilizing effects on different protein domains. Notably, it has a broad spectrum of GPCR activities, showing positive modulation on GPR119 (2.783% maximal response), and inhibitory effects on CX3CR1, ADRB2, APLNR, FPR2, ADRA2A, C5AR1, and S1PR1 among others, with varying levels of inhibition. Furthermore, it exhibits both maximal response and inhibition at different concentrations on targets like FFAR4, AGTR1, GPR35, and GLP1R, thus highlighting its extensive and diverse bioactivity profile..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	PF-06291874 (Glucagon receptor antagonists-4) (Glucagon receptor antagonists-4) is a highly effective and orally active antagonist of the glucagon receptor.
Synonyms	Glucagon receptor antagonists-4

Chemical Properties

Molecular Weight	503.51
Formula	C₂₆H₂₈F₃N₃O₄
Cas No.	1393124-08-7
Smiles	CCC[C@H](Oc1cc(C)c(c(C)c1)-n1cc(cn1)C(F)(F)F)c1ccc(cc1)C(=O)NCCC(O)=O
Relative Density.	1.27 g/cm3 (Predicted)

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 30 mg/mL (59.58 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.97 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	1.9861 mL	9.9303 mL	19.8606 mL	99.3029 mL
5 mM	0.3972 mL	1.9861 mL	3.9721 mL	19.8606 mL
10 mM	0.1986 mL	0.9930 mL	1.9861 mL	9.9303 mL
20 mM	0.0993 mL	0.4965 mL	0.9930 mL	4.9651 mL
50 mM	0.0397 mL	0.1986 mL	0.3972 mL	1.9861 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