Ketohexokinase inhibitor 1 |
| Catalog No.GC31400 |
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2102501-84-6
Sample solution is provided at 25 µL, 10mM.
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Ketohexokinase inhibitor 1 is an inhibitor of ketohexokinase (KHK), with IC50s of 8.4 nM and 66 nM for KHK-C and KHK-A, respectively, extracted from patent US 20170183328 A1, example 4.
Ketohexokinase inhibitor 1 (Example 4) is an inhibitor of ketohexokinase (KHK), with IC50s of 8.4 nM and 66 nM for KHK-C and KHK-A, sepctively[1].
[1]. SUBSTITUTED 3-AZABICYCLO[3.1.0]HEXANES AS KETOHEXOKINASE INHIBITORS. US 20170183328 A1
Kinase experiment: | A 384-well format on a assay plate is used in the assay and monitored by UV-vis spectroscopy in continuous mode at room temperature (rt). Compounds (Ketohexokinase inhibitor 1) are prepared in DMSO as 4 mM stocks, diluted using an 11-point half-log scheme on a Biomek FX, and incubated at rt for 30 minutes with the reaction mixture containing 50 mM HEPES, pH 7.4, 140 mM KCl, 3.5 mM MgCl2, 0.8 mM fructose, 2 mM TCEP, 0.8 mM PEP, 0.7 mM NADH, 0.01% Triton X-100, 30 U/mL pyruvate kinase-lactate dehydrogenase, and 10 nM purified KHK-C. The compound concentration in each well ranged from 1 nM to 100 μM. The reaction is initiated with the addition of 0.2 mM ATP. The absorbance is measured for 30 minutes on a SpectraMax reader after ATP is added. The concentrations provided are based on the final mixture volume of 40 μL[1]. |
References: [1]. SUBSTITUTED 3-AZABICYCLO[3.1.0]HEXANES AS KETOHEXOKINASE INHIBITORS. US 20170183328 A1 | |
| Cas No. | 2102501-84-6 | SDF | |
| Canonical SMILES | O=C(C[C@H]1[C@@]2(CN(C[C@]12[H])C3=NC(N4[C@H](CC4)C)=NC(C(F)(F)F)=C3)[H])O | ||
| Formula | C16H19F3N4O2 | M.Wt | 356.34 |
| Solubility | DMS : ≥ 125 mg/mL (350.79 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. |
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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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8063 mL | 14.0315 mL | 28.0631 mL |
| 5 mM | 0.5613 mL | 2.8063 mL | 5.6126 mL |
| 10 mM | 0.2806 mL | 1.4032 mL | 2.8063 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 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.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 26 reference(s) in Google Scholar.)
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