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PF-07258669

Name: PF-07258669
Brand: TargetMol
SKU: T69526
Price: 1690 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T69526 Copy Product Info

Purity: 99.9%

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PF-07258669 is a small-molecule compound and a melanocortin 4 receptor (MC4R) antagonist (IC50 = 13 nM, Ki = 0.46 nM) with high selectivity, oral bioavailability, and favorable pharmacokinetic properties. This compound can be used for research on diseases such as cachexia and anorexia.

Cas No. 2755890-53-8

Pack Size	Price	USA Stock	Global Stock
1 mg	$845	In Stock	In Stock
5 mg	$1,690	In Stock	In Stock
10 mg	Inquiry	In Stock	In Stock
25 mg	Inquiry	In Stock	In Stock
50 mg	Inquiry	Inquiry	Inquiry

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.9%

ee:96.54%

Appearance:Solid

Color:Yellow

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COA CSFC FNMR HNMR LCMS

Product Introduction

Bioactivity

Description	PF-07258669 is a small-molecule compound and a melanocortin 4 receptor (MC4R) antagonist (IC50 = 13 nM, Ki = 0.46 nM) with high selectivity, oral bioavailability, and favorable pharmacokinetic properties. This compound can be used for research on diseases such as cachexia and anorexia.
In vitro	Methods: The in vitro activity of PF-07258669 was evaluated in CHO cells stably expressing hMC4R through [¹²⁵I]NDP-α MSH competitive binding assays and cAMP functional assays. Results: PF-07258669 exhibited high affinity for hMC4R (Ki=0.46 nM) and potent antagonist activity (Kb=0.72 nM), with high affinity also observed for rat and canine MC4R (Ki=0.52 nM and 0.094 nM, respectively). The compound showed lower selectivity for hMC3R and hMC5R (Ki=340 nM and 840 nM, respectively) and no significant binding to hMC1R. [1]
In vivo	Methods: To evaluate the pharmacodynamic and pharmacokinetic properties of PF-07258669, aged rats were administered PF-07258669 (0.3–10 mg/kg, oral, twice daily for 22 days), and its effects on appetite, food intake, and body weight were observed; pharmacokinetic parameters were also determined in rats and dogs. Results: PF-07258669 modulated appetite and increased daily food intake and body weight in aged rat models; pharmacokinetic properties were favorable in rats and dogs, with oral bioavailability of 93% in dogs. [1]

Chemical Properties

Molecular Weight	462.52
Formula	C₂₅H₂₇FN₆O₂
Cas No.	2755890-53-8
Smiles	C([C@H](C)C=1C=C(OC)N=CC1F)(=O)N2C[C@@]3(NC=4C(CC3)=CC(=C(C)N4)C=5N=CC=CN5)CC2

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.

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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