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PF-05105679

🥰Excellent
Catalog No. T16483Cas No. 1398583-31-7

PF-05105679 is a selective TRPM8 antagonist (IC50 = 103 nM). PF-05105679 can be used in research on cold-related pain.

PF-05105679

PF-05105679

🥰Excellent
Purity: 99.84%
Catalog No. T16483Cas No. 1398583-31-7
PF-05105679 is a selective TRPM8 antagonist (IC50 = 103 nM). PF-05105679 can be used in research on cold-related pain.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$40In StockIn Stock
5 mg$94In StockIn Stock
10 mg$157In StockIn Stock
25 mg$315In StockIn Stock
50 mg$473In StockIn Stock
100 mg$712In StockIn Stock
200 mg$983In StockIn Stock
1 mL x 10 mM (in DMSO)$97In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.84%
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Product Introduction

Bioactivity
Description
PF-05105679 is a selective TRPM8 antagonist (IC50 = 103 nM). PF-05105679 can be used in research on cold-related pain.
Targets&IC50
TRPM8:103 nM
In vitro
PF-05105679 shows >100-fold selectivity across a range of different receptors, ion channels, and enzymes including the closely related TRPV1 and TRPA1 channels[1].
In vivo
PF-05105679 (2, 20 mg/kg) shows a T1/2 of 3.6 hours, a CL of 19.8 mL/min/kg, and a Vss of 6.2 L/kg for rats. PF-05105679 (0.2 mg/kg for iv and 20mg/kg for oral gavage) displays a T1/2 of 3.9 hours, a CL of 31 mL/min/kg, and a Vss of 7.4 L/kg for dogs[1].
Chemical Properties
Molecular Weight428.45
FormulaC26H21FN2O3
Cas No.1398583-31-7
SmilesC[C@@H](N(Cc1cccc(c1)C(O)=O)C(=O)c1cnc2ccccc2c1)c1ccc(F)cc1
Relative Density.1.308 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 120 mg/mL (280.08 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (9.34 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
1mg5mg10mg50mg
1 mM2.3340 mL11.6700 mL23.3399 mL116.6997 mL
5 mM0.4668 mL2.3340 mL4.6680 mL23.3399 mL
10 mM0.2334 mL1.1670 mL2.3340 mL11.6700 mL
20 mM0.1167 mL0.5835 mL1.1670 mL5.8350 mL
50 mM0.0467 mL0.2334 mL0.4668 mL2.3340 mL
100 mM0.0233 mL0.1167 mL0.2334 mL1.1670 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 mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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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

Keywords

TRPVChannelTRPV ChannelTRPM8TRPChannelTRP ChannelTransient receptor potential channelssubfamilyPF-05105679PF05105679PF 05105679painorallymentholmelastatinInhibitorinhibitcold-relatedcoldCMR1clinical
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