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Arhalofenate

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Catalog No. T16022Cas No. 24136-23-0
Alias MBX 102, JNJ 39659100

Arhalofenate (JNJ 39659100) is a selective partial agonist of peroxisome proliferator-activated receptor PPARγ. It is used for the treatment of type 2 diabetes.

Arhalofenate

Arhalofenate

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Purity: 98.97%
Catalog No. T16022Alias MBX 102, JNJ 39659100Cas No. 24136-23-0
Arhalofenate (JNJ 39659100) is a selective partial agonist of peroxisome proliferator-activated receptor PPARγ. It is used for the treatment of type 2 diabetes.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$56In StockIn Stock
5 mg$215In StockIn Stock
10 mg$378In StockIn Stock
25 mg$619In StockIn Stock
50 mg$868In StockIn Stock
100 mg$1,170In StockIn Stock
200 mg$1,580In StockIn Stock
1 mL x 10 mM (in DMSO)$285In 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:98.97%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Arhalofenate (JNJ 39659100) is a selective partial agonist of peroxisome proliferator-activated receptor PPARγ. It is used for the treatment of type 2 diabetes.
In vitro
Arhalofenate displays a dose-dependent activation of mouse GAL4-PPAR-γ (EC50s: appr 12 μM). Arhalofenate is a prodrug ester, that is rapidly and completely modified in vivo by non-specific serum esterases to the mature free acid form Arhalofenate (MBX 102) acid. [2].
In vivo
MBX-102 significantly reduces fasting blood glucose, confirming that Arhalofenate (MBX 102) is an efficacious antidiabetic agent. Arhalofenate (60 mg/kg) causes a dramatic decrease in plasma and also results in a dose-dependent, significant decrease in the insulin resistance indexinsulin levels[1]. Arhalofenate (100 mg/kg, p.o.) obviously increases the glucose infusion rate and decreases hepatic glucose output in the clamped state in Zucker Diabetic Fatty (ZDF) rats. Arhalofenate (100 mg/kg, p.o.) significantly reduces triglyceride, free fatty acid, and cholesterol levels in ZDF rats. Arhalofenate (100 mg/kg, p.o.) also significantly lowers fasting plasma insulin, and robustly decreases fasting plasma triglycerides after 32 days of treatment in Zucker Fatty (ZF) rats[2].
SynonymsMBX 102, JNJ 39659100
Chemical Properties
Molecular Weight415.79
FormulaC19H17ClF3NO4
Cas No.24136-23-0
Smiles[C@H](OC1=CC(C(F)(F)F)=CC=C1)(C(OCCNC(C)=O)=O)C2=CC=C(Cl)C=C2
Relative Density.1.331 g/cm3
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: 132.5 mg/mL (318.67 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.4051 mL12.0253 mL24.0506 mL120.2530 mL
5 mM0.4810 mL2.4051 mL4.8101 mL24.0506 mL
10 mM0.2405 mL1.2025 mL2.4051 mL12.0253 mL
20 mM0.1203 mL0.6013 mL1.2025 mL6.0127 mL
50 mM0.0481 mL0.2405 mL0.4810 mL2.4051 mL
100 mM0.0241 mL0.1203 mL0.2405 mL1.2025 mL

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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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
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2 Enter the in vivo formulation:
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