MAP4K4-IN-3 |
カタログ番号GC63059
One-Click Copy Product Info
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MAP4K4-IN-3 (化合物 17) は、キナーゼアッセイで 14.9 nM の IC50、細胞アッセイで 470 nM の IC50 を持つ強力かつ選択的な MAP4K4 阻害剤です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1811510-58-3
Sample solution is provided at 25 µL, 10mM.
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MAP4K4-IN-3 (Compound 17) is a potent and selective MAP4K4 inhibitor with an IC50 of 14.9 nM in kinase assay, an IC50 of 470 nM in cell assay. Antidiabetic agent[1].
MAP4K4, a serine/threonine protein kinase may be a viable target for antidiabetic agents[1].
Oral dosing in telemetered rats for 5 days with MAP4K4-IN-3 (Compound 2; 25 mg/kg, b.i.d.) results in a number of adverse effects. Substantial weight losses (7%) and body temperature increases (0.4°C) relative to controls are observed over the course of the study. For cardiovascular end points, maximal heart rate increases of 25 bpm, relative to controls, are induced by treatment with MAP4K4-IN-3[2].
[1]. Ammirati M, et al. Discovery of an in Vivo Tool to Establish Proof-of-Concept for MAP4K4-Based AntidiabeticTreatment. ACS Med Chem Lett. 2015 Oct 6;6(11):1128-33.
[2]. Dow RL, et al. 2-Aminopyridine-Based Mitogen-Activated Protein Kinase Kinase Kinase Kinase 4 (MAP4K4) Inhibitors: Assessment of Mechanism-Based Safety. J Med Chem. 2018 Apr 12;61(7):3114-3125.
| Cas No. | 1811510-58-3 | SDF | |
| Formula | C15H12ClN5 | M.Wt | 297.74 |
| 溶解度 | DMSO : 10 mg/mL (33.59 mM; ultrasonic and warming and heat to 60°C) | Storage | 4°C, protect from light |
| 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.3586 mL | 16.7932 mL | 33.5864 mL |
| 5 mM | 671.7 μL | 3.3586 mL | 6.7173 mL |
| 10 mM | 335.9 μL | 1.6793 mL | 3.3586 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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 saline, 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.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)