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APD668

Name: APD668
Brand: TargetMol
SKU: T2088
Price: 45 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T2088Cas No. 832714-46-2

Alias APD 668

APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119, respectively.

APD668

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Purity: 99.97%

Catalog No. T2088Alias APD 668Cas No. 832714-46-2

APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119, respectively.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$45	In Stock	In Stock
5 mg	$106	In Stock	In Stock
10 mg	$163	In Stock	In Stock
25 mg	$297	In Stock	In Stock
50 mg	$488	In Stock	In Stock
100 mg	$689	-	In Stock
1 mL x 10 mM (in DMSO)	$117	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:99.97%

Appearance:Solid

Color:White

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COA HPLC HNMR

Product Introduction

APD668 AI Summary

APD668 exhibits a range of bioactivities including notable pharmacological and biochemical properties. It demonstrates potent inhibition of CYP2C9 with a Ki value of 100.0 nM and exhibits agonist activity at human and rat GPR119, with EC50 values of 2.7 nM and 33.0 nM, respectively. In ZDF rat models, it shows antidiabetic activity by reducing glycated hemoglobin and blood glucose levels. The compound has favorable oral bioavailability and a selectivity ratio of EC50, indicating selective activity on GPR119. Pharmacokinetic studies reveal varying clearance rates across animal models: 3.833 mL.min-1.kg-1 in Swiss albino mice, 20.0 mL.min-1.kg-1 in Sprague-Dawley rats, 7.333 mL.min-1.kg-1 in Zucker fa/fa rats, 2.0 mL.min-1.kg-1 in Beagle dogs, and 1.833 mL.min-1.kg-1 in Cynomolgus monkeys, which suggests species-specific metabolic behaviors. The LogD7.4 value of 3.0 indicates high lipophilicity and potential for membrane permeability, and the moderate solubility in pH 7.4 buffer (2100.0 nM) may influence its formulation and bioavailability. APD668 has demonstrated antiviral properties, inhibiting the cytotoxicity induced by SARS-CoV-2 in Caco-2 cells at 10 µM with a 24.13% inhibition rate and showing SARS-CoV-2 3CL-Pro protease inhibition at 20 µM concentrations (8.79% and 22.19% inhibition). It also inhibits SARS-CoV-2-induced cytotoxicity in VERO-6 cells at the same concentration. Additionally, APD668 exhibits inhibitory activity in human HDAC6 enzymatic assays, stronger with commercial peptide substrates (22.09%) than with custom ones (2.8%). It affects cell growth variably, inhibiting U2OS cell growth while promoting viability in human fibroblast and HEK293T cells. Thermal Shift Assays indicate it impacts thermal stability across different protein domains, suggesting interactions with protein stability. In GPCR beta-arrestin recruitment assays, APD668 displays both agonistic and inhibitory effects on various receptors, indicating multifunctional GPCR activity. This versatility highlights its potential as a compound with diverse therapeutic applications..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119, respectively.
Targets&IC50	GPR119 (rat):33 nM (EC50), GPR119 (human):2.7 nM (EC50), CYP2C9:0.1 μM (Ki), ERG channel (human):3 μM
Synonyms	APD 668

Chemical Properties

Molecular Weight	477.51
Formula	C₂₁H₂₄FN₅O₅S
Cas No.	832714-46-2
Smiles	CC(C)OC(=O)N1CCC(CC1)Oc1ncnc2n(ncc12)-c1ccc(cc1F)S(C)(=O)=O
Relative Density.	1.47 g/cm3 (Predicted)

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 45 mg/mL (94.24 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0942 mL	10.4710 mL	20.9420 mL	104.7098 mL
5 mM	0.4188 mL	2.0942 mL	4.1884 mL	20.9420 mL
10 mM	0.2094 mL	1.0471 mL	2.0942 mL	10.4710 mL
20 mM	0.1047 mL	0.5235 mL	1.0471 mL	5.2355 mL
50 mM	0.0419 mL	0.2094 mL	0.4188 mL	2.0942 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