LIQ1
Based on 1 Customer Validation
LIQ1, a flavonoid derivative, is a potent Pyruvate kinase M2 (PKM2) allosteric inhibitor (IC50 = 0.39 μM; Kd = 4.5 μM) targeting Arg43 within the polyarginine pocket. LIQ1 exhibits efficacy in a mouse model of LPS (HY-D1056)-induced endotoxemia, preventing the nuclear translocation of PKM2 and inhibiting its binding to HIF-1α, thereby suppressing IL-1β transcription. LIQ1 can be used for the research of endotoxemia[1].
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- Pureza: 97.40%
- No. CAS: 2606032-80-6
- Fòrmula: C16H12O5
- Peso molecular:284.26
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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PKM2 0.39 μM (IC50) |
PKM2 4.5 μM (Kd) |
LIQ1 (100 μM; 2 h) significantly enhances the thermal stability of PKM2 within the tem-perature range of 40-52 °C, increasing its melting temperature (Tm) by 3.4 °C[1].
LIQ1 significantly reduces the inhibitory effect on PKM2 R43A (IC50 = 4.10 μM; Kd = 11.1 μM) compared to wild-type PKM2 (IC50 = 0.98 μM; Kd = 3.2 μM), indicating that R43 is a critical residue mediating the allosteric inhibition of PKM2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
LIQ1 (20 mg/kg; i.p.; single dose or daily for 14 days) shows negligible acute toxicity and no hepatorenal toxicity in mice, supporting its favorable safety profile[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male BALB/c mice (6-8 weeks old) intraperitoneally injected with LPS (13 mg/kg)[1]
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Dosage:1, 2, 5 mg/kg
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Administration:i.p.; administered at 0, 12, 24, and 36 h after LPS injection
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Result:Increased the 7-day survival rate from 40% (1 mg/kg) to 80% (5 mg/kg).
Exhibited a dose-dependent reduction in serum IL-1β levels.
Mitigated the injuries induced by LPS, such as microvilli loss, villus atrophy, deformation, and necrosis.
Alleviated the LPS-induced pathological lesions in the lung and heart tissues at the dose of 5 mg/kg.
Suppressed LPS-induced ATP accumulation.
Significantly inhibited the nuclear translocation of PKM2 in the small intestine, lung, and heart tissues.
Prevented PKM2-HIF-1α complex formation, ultimately leading to reduced IL-1β transcription in mice.
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Animal Model:Male BALB/c mice (6-8 weeks old)[1]
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Dosage:20 mg/kg
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Administration:i.p.; single dose
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Result:Showed no significant decrease in body weight over 14 days.
Revealed no changes in motor activity, grooming and rubbing behaviors.
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Animal Model:Male BALB/c mice (6-8 weeks old)[1]
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Dosage:20 mg/kg
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Administration:i.p.; daily for 14 days
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Result:Revealed a significant increase in alkaline phosphatase (ALP) levels.
Showed no statistically significant changes in other liver enzymes, including AST, ALT, GGT, total protein (TP), albumin (ALB), and globulin (GLO).
Showed no significant effects on kidney function parameters, including urea, creatinine (CREA), uric acid (UA), and estimated glomerular filtration rate (eGFR).
Chemical Information
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No. CAS 2606032-80-6
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Appearance Solid
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Peso molecular 284.26
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Fòrmula C16H12O5
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Color White to off-white
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SMILES
O=C(C1=CC=CC=C1C2CC(C3=CC=C(C=C3O2)O)=O)O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 33.33 mg/mL (117.25 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)
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: ≥ 2.5 mg/mL (8.79 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.79 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 3.5179 mL | 17.5895 mL | 35.1791 mL | 87.9477 mL |
| 5 mM | 0.7036 mL | 3.5179 mL | 7.0358 mL | 17.5895 mL | |
| 10 mM | 0.3518 mL | 1.7590 mL | 3.5179 mL | 8.7948 mL | |
| 15 mM | 0.2345 mL | 1.1726 mL | 2.3453 mL | 5.8632 mL | |
| 20 mM | 0.1759 mL | 0.8795 mL | 1.7590 mL | 4.3974 mL | |
| 25 mM | 0.1407 mL | 0.7036 mL | 1.4072 mL | 3.5179 mL | |
| 30 mM | 0.1173 mL | 0.5863 mL | 1.1726 mL | 2.9316 mL | |
| 40 mM | 0.0879 mL | 0.4397 mL | 0.8795 mL | 2.1987 mL | |
| 50 mM | 0.0704 mL | 0.3518 mL | 0.7036 mL | 1.7590 mL | |
| 60 mM | 0.0586 mL | 0.2932 mL | 0.5863 mL | 1.4658 mL | |
| 80 mM | 0.0440 mL | 0.2199 mL | 0.4397 mL | 1.0993 mL | |
| 100 mM | 0.0352 mL | 0.1759 mL | 0.3518 mL | 0.8795 mL |
LIQ1 Related Classifications
HY-179371 Related Classifications
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