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M77976

Catalog No.GC60232

M77976 is a specific ATP-competitive inhibitor of PDK4 (pyruvate dehydrogenase kinase isoforms 4), with an IC50 of 648 μM.

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M77976 Chemical Structure

Cas No.: 394237-61-7

Size Price Stock Qty
10mM (in 1mL DMSO)
$97.00
In stock
1mg
$40.00
In stock
5mg
$77.00
In stock
10mg
$126.00
In stock
25mg
$245.00
In stock
50mg
$371.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Description of M77976

M77976 is a specific ATP-competitive inhibitor of PDK4 (pyruvate dehydrogenase kinase isoforms 4), with an IC50 of 648 μM. M77976 is potential for the research of obesity and diabetes[1].

M77976 binds to the ATP-binding pocket of PDK4 and causes local conformational changes with complete disordering of the ATP lid[1].M77976 makes hydrophobic interactions with the side chains of Asn258, Ala262, Val298, Leu306 and Thr358 of PDK4[1].

[1]. Kukimoto-Niino M, et al. Inhibitor-bound structures of human pyruvate dehydrogenase kinase 4. Acta Crystallogr D Biol Crystallogr. 2011 Sep;67(Pt 9):763-73.

Chemical Properties of M77976

Cas No. 394237-61-7 SDF
Canonical SMILES COC1=CC=C(C=C1)C2=C(NN=C2C3=CC=C(C=C3O)O)C
Formula C17H16N2O3 M.Wt 296.32
Solubility DMSO: 250 mg/mL (843.68 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of M77976

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 3.3747 mL 16.8737 mL 33.7473 mL
5 mM 0.6749 mL 3.3747 mL 6.7495 mL
10 mM 0.3375 mL 1.6874 mL 3.3747 mL
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In vivo Formulation Calculator (Clear solution) of M77976

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 3 reference(s) in Google Scholar.)

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