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APD597

Name: APD597
Brand: TargetMol
SKU: T3176
Price: 64 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T3176Cas No. 897732-93-3

Alias JNJ-38431055

APD597 (JNJ-38431055) is a GPR119 agonist, used in the treatment of type 2 diabetes.

APD597

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Purity: 99.78%

Catalog No. T3176Alias JNJ-38431055Cas No. 897732-93-3

APD597 (JNJ-38431055) is a GPR119 agonist, used in the treatment of type 2 diabetes.

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$64	In Stock	In Stock
10 mg	$113	In Stock	In Stock
25 mg	$179	In Stock	In Stock
50 mg	$239	In Stock	In Stock
100 mg	$372	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$67	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:99.78%

Color:White

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Product Introduction

APD597 AI Summary

APD597 exhibits a diverse range of bioactivities and pharmacological profiles. It acts as an agonist at human and rat GPR119 receptors with EC50 values of 46.0 nM and 421.0 nM, respectively, and demonstrates moderate intrinsic activity at the human receptor (75.0% relative to AR231453) while displaying high intrinsic activity at the rat receptor (89.0% relative to AR231453). The compound also inhibits CYP2C9 with an IC50 of 8000.0 nM and shows moderate oral bioavailability in Sprague-Dawley rats (72.0%) and cynomolgus monkeys (68.8%). In various animal models, APD597 highlights its antidiabetic potential by significantly reducing blood glucose levels. It presents a favorable pharmacokinetic profile with acceptable half-lives and demonstrates good drug uptake and limited metabolism (less than 20.0% conversion to metabolite) in oral dosed rats. Its intrinsic clearance rates in rat hepatocytes and human liver microsomes are CL 6.31 µL.min^-1.(10^6 cells)^-1 and CL 19.95 mL.min^-1.g^-1, respectively, and it has a solubility of 14800.0 nM in a pH 7.4 buffer with a LogD7.4 of 2.4. Additionally, APD597 shows some anti-SARS-CoV-2 activity, evidenced by a modest inhibition of SARS-CoV-2 induced cytotoxicity in Caco-2 and VERO-6 cells, and inhibition of SARS-CoV-2 3CL-Pro protease. The compound also exhibits moderate inhibitory activity against human HDAC6. In cellular assays, APD597 impacts growth rates differently across multiple cell lines, including human fibroblasts, HEK293T cells, and U2OS cells. Thermal shift assays indicate that it has varying effects on protein stability, suggesting interactions with different protein domains. Moreover, it modulates multiple GPCRs, displaying both agonistic and inhibitory activities in beta-arrestin recruitment assays. Overall, APD597 emerges as a multifunctional compound with potential applications in metabolic disorders, antiviral therapy, and broader pharmacological contexts involving GPCR signaling pathways and protein stability modulation..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	APD597 (JNJ-38431055) is a GPR119 agonist, used in the treatment of type 2 diabetes.
Targets&IC50	GPR119 (human):46 nM
Synonyms	JNJ-38431055

Chemical Properties

Molecular Weight	479.55
Formula	C₂₁H₂₉N₅O₆S
Cas No.	897732-93-3
Smiles	COc1c(Nc2ccc(nc2C)S(C)(=O)=O)ncnc1OC1CCN(CC1)C(=O)OC(C)C
Relative Density.	1.311 g/cm3 (Predicted)

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: 60 mg/mL (125.12 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.17 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	2.0853 mL	10.4264 mL	20.8529 mL	104.2644 mL
5 mM	0.4171 mL	2.0853 mL	4.1706 mL	20.8529 mL
10 mM	0.2085 mL	1.0426 mL	2.0853 mL	10.4264 mL
20 mM	0.1043 mL	0.5213 mL	1.0426 mL	5.2132 mL
50 mM	0.0417 mL	0.2085 mL	0.4171 mL	2.0853 mL
100 mM	0.0209 mL	0.1043 mL	0.2085 mL	1.0426 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