LI-2242
Based on 1 Customer Validation
LI-2242 is an inositol hexakisphosphate kinase (IP6K) inhibitor. LI-2242 has inhibition effect for IP6K1, IP6K2, IP6K3 and IPMK with IC50 values of 31 nM, 42 nM, 8.7 nM and 1944 nM, respectively. LI-2242 can be used for thew research of type II diabetes, obesity, metabolic complications, venous thrombosis, and psychiatric disorders.
For research use only. We do not sell to patients.
- Purity : 98.83%
- CAS No.: 2762762-17-2
- Formula: C20H18Cl2N2O3
- Molecular Weight:405.27
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Description
IC50 & Target
IC50: 31 nM (IP6K1); 42 nM (IP6K2); 8.7 nM (IP6K3); 1944 nM (IPMK)[1].
In Vitro
LI-2242 has inhibition effect for IP6K1, IP6K2, IP6K3 and IPMK with IC50 values of 31 nM, 42 nM, 8.7 nM and 1944 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 2762762-17-2
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Appearance Solid
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Molecular Weight 405.27
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Formula C20H18Cl2N2O3
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Color White to off-white
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SMILES
O=C(C1=CC=C2NC(C3(CCN(CC3)CC4=CC=C(C=C4Cl)Cl)C2=C1)=O)O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 200 mg/mL (493.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (12.34 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
Purity & Documentation
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4675 mL | 12.3375 mL | 24.6749 mL | 61.6873 mL |
| 5 mM | 0.4935 mL | 2.4675 mL | 4.9350 mL | 12.3375 mL | |
| 10 mM | 0.2467 mL | 1.2337 mL | 2.4675 mL | 6.1687 mL | |
| 15 mM | 0.1645 mL | 0.8225 mL | 1.6450 mL | 4.1125 mL | |
| 20 mM | 0.1234 mL | 0.6169 mL | 1.2337 mL | 3.0844 mL | |
| 25 mM | 0.0987 mL | 0.4935 mL | 0.9870 mL | 2.4675 mL | |
| 30 mM | 0.0822 mL | 0.4112 mL | 0.8225 mL | 2.0562 mL | |
| 40 mM | 0.0617 mL | 0.3084 mL | 0.6169 mL | 1.5422 mL | |
| 50 mM | 0.0493 mL | 0.2467 mL | 0.4935 mL | 1.2337 mL | |
| 60 mM | 0.0411 mL | 0.2056 mL | 0.4112 mL | 1.0281 mL | |
| 80 mM | 0.0308 mL | 0.1542 mL | 0.3084 mL | 0.7711 mL | |
| 100 mM | 0.0247 mL | 0.1234 mL | 0.2467 mL | 0.6169 mL |