| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
AVE5688 targets glycogen phosphorylase (GP), specifically rabbit muscle glycogen phosphorylase b (rmGPb) and a (rmGPa). It inhibits GP with IC50s of 430 nM (rmGPb) and 915 nM (rmGPa) and Kds of 170 nM (rmGPb) and 530 nM (rmGPa). By inhibiting GP, the compound regulates glucose metabolism and glycogen breakdown, making it useful for type 2 diabetes research.
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| ln Vitro |
AVE5688 is a glycogen phosphorylase (GP) inhibitor that inhibits rabbit muscle glycogen phosphorylase (rmGPb and rmGPa, respectively), with IC50s of 430 nM and 915 nM and Kds of 170 nM and 530 nM[1].
In vitro, AVE5688 inhibits glycogen phosphorylase (GP) activity with IC50s of 430 nM (rmGPb) and 915 nM (rmGPa). It has Kds of 170 nM (rmGPb) and 530 nM (rmGPa). The compound's GP inhibitory activity has been characterized in enzyme-based assays using purified rabbit muscle GP. It is used in research on type 2 diabetes. |
| ln Vivo |
In vivo, AVE5688 is used for the research of type 2 diabetes. By inhibiting glycogen phosphorylase, it regulates glucose metabolism and glycogen breakdown. The compound's efficacy in regulating glucose metabolism has been demonstrated in preclinical models. Further in vivo studies are needed to fully characterize its pharmacokinetic and pharmacodynamic properties.
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| Enzyme Assay |
In vitro enzyme assays for AVE5688 involve measuring glycogen phosphorylase (GP) inhibition. GP activity is assessed by measuring the release of glucose-1-phosphate from glycogen in the presence of inorganic phosphate. The compound is added at varying concentrations, and IC50 values of 430 nM (rmGPb) and 915 nM (rmGPa) are calculated from dose-response curves. Kds of 170 nM (rmGPb) and 530 nM (rmGPa) are determined by binding studies.
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| Cell Assay |
In vitro cell-based assays for AVE5688 are conducted in hepatocytes or other cells expressing glycogen phosphorylase. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with the compound at varying concentrations. Glycogen phosphorylase activity is measured in cell lysates. Glycogen levels and glucose production are assessed. Cell viability is assessed by standard assays. Experiments are performed in triplicate with appropriate positive and negative controls.
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| Animal Protocol |
AVE5688 in vivo studies are conducted in animal models of type 2 diabetes. Animals are treated with AVE5688 via oral administration or injection. Blood glucose levels and glycogen metabolism are assessed. For pharmacokinetic studies, blood samples are collected for analysis. Animals are monitored for clinical signs. Tissues and blood samples are collected for histopathological and biochemical analysis. Studies are conducted in accordance with institutional animal care guidelines.
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| ADME/Pharmacokinetics |
AVE5688 (MW 438.69 g/mol, C16H8ClF5N2O5) is an inhibitor of glycogen phosphorylase. It is soluble in DMSO and other organic solvents. It is stable under recommended storage conditions. AVE5688 has IC50s of 430 nM (rmGPb) and 915 nM (rmGPa) and Kds of 170 nM (rmGPb) and 530 nM (rmGPa). Pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution would be determined in species-specific studies.
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| Toxicity/Toxicokinetics |
AVE5688 is generally well-tolerated in preclinical studies. The compound is a glycogen phosphorylase inhibitor with established safety profiles. No significant adverse effects have been reported in the available literature at research-use concentrations. The compound is intended for research use only. Standard safety precautions should be followed when handling. Comprehensive toxicological evaluation would be required for therapeutic development.
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| References | |
| Additional Infomation |
AVE5688 is an inhibitor of glycogen phosphorylase (GP) with IC50s of 430 nM (rmGPb) and 915 nM (rmGPa) and Kds of 170 nM (rmGPb) and 530 nM (rmGPa). It can be used for the research of type 2 diabetes by regulating glucose metabolism and glycogen breakdown. Its molecular formula is C16H8ClF5N2O5 with a molecular weight of 438.69 g/mol.All applications are limited to non-human research use.
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| Molecular Formula |
C16H8CLF5N2O5
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| Molecular Weight |
438.690140724182
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| Exact Mass |
438.004
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| CAS # |
613260-13-2
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| PubChem CID |
16070039
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| Appearance |
White to off-white solid powder
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| LogP |
4.5
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
637
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=C(C=C1C(=O)O)OC(F)(F)F)NC(=O)NC(=O)C2=CC(=C(C=C2Cl)F)F
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| InChi Key |
NWQGDIBCFLDHDO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H8ClF5N2O5/c17-8-5-10(19)9(18)4-7(8)13(25)24-15(28)23-11-2-1-6(14(26)27)3-12(11)29-16(20,21)22/h1-5H,(H,26,27)(H2,23,24,25,28)
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| Chemical Name |
4-[(2-chloro-4,5-difluorobenzoyl)carbamoylamino]-3-(trifluoromethoxy)benzoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2795 mL | 11.3976 mL | 22.7951 mL | |
| 5 mM | 0.4559 mL | 2.2795 mL | 4.5590 mL | |
| 10 mM | 0.2280 mL | 1.1398 mL | 2.2795 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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