Iminostilbene
Based on 1 Customer Validation
Iminostilbene is a chemical precursor of carbamazepine. Additionally, Iminostilbene is an orally active inhibitor of PKM2 (Pyruvate Kinase M2) and COX2 (Cyclooxygenase-2). Iminostilbene exerts its effects by inhibiting PKM2 and its interaction with HIF-1α and STAT3, reducing COX2 and iNOS expression, and decreasing LPS-induced release of IL-1β, IL-6, TNF-α, and MCP-1, thereby suppressing macrophage-mediated inflammatory responses and improving myocardial ischemia/reperfusion (MI/R) injury. Iminostilbene holds promise for research in inflammation regulation, cardiovascular diseases (such as MI/R injury), and macrophage-mediated immune-related diseases.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.66%
- No. CAS: 256-96-2
- Fòrmula: C14H11N
- Peso molecular:193.25
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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Ver todos los productos específicos de isoformas TNF Receptor
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Actividad biológica
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COX-2 |
iNOS |
STAT3 |
HIF-1α |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U-937 | IC50 |
2.58 μM
Compound: 11
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Cytotoxicity in UV-irradiated human U937 cells exposed to photosensitizer for 2 hrs before irradiation for 20 mins by WST-1 assay
Cytotoxicity in UV-irradiated human U937 cells exposed to photosensitizer for 2 hrs before irradiation for 20 mins by WST-1 assay
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[PMID: 24900465] |
Iminostilbene (2.5-10 μM, 30 h) inhibits LPS-induced inflammatory response, reduces PKM2 expression, and suppresses its downstream signaling pathways in RAW264.7 macrophages[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LPS (HY-D1056)-induced RAW264.7 macrophages (mouse-derived)
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Concentration:2.5 μM, 5 μM, 10 μM
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Incubation Time:30 h (6 h pre-treatment with Iminostilben, followed by LPS stimulation for 24 h)
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Result:Showed no significant effect on cell viability at low doses, slight reduction at high dose (10 μM).
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Cell Line:LPS (HY-D1056)-induced RAW264.7 macrophages (mouse-derived)
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Concentration:2.5 μM, 5 μM, 10 μM
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Incubation Time:30 h (6 h pre-treatment with Iminostilben, followed by LPS stimulation for 24 h)
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Result:Suppressed IL-1β, IL-6, MCP-1, and TNF-α mRNA levels.
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Cell Line:LPS (HY-D1056)-induced RAW264.7 macrophages (mouse-derived)
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Concentration:2.5 μM, 5 μM, 10 μM
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Incubation Time:30 h (6 h pre-treatment with Iminostilben, followed by LPS stimulation for 24 h)
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Result:Inhibited COX2, PKM2, and iNOS protein expression and reduced PKM2-HIF-1α-STAT3 interaction.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Myocardial ischemia/reperfusion (MI/R) injury Sprague-Dawley (SD) rat model[2]
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Dosage:0.625 mg/kg, 1.25 mg/kg
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Administration:Oral gavage (p.o.), once daily for 5 days
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Result:Improved cardiac function, reduced myocardial infarction area. Decreased CK-MB, LDH, and cTnT levels. Reduced inflammatory cell infiltration, inhibited COX2 and iNOS expression, and suppressed IL-1β and IL-6 RNA and protein levels.
Chemical Information
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No. CAS 256-96-2
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Appearance Solid
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Peso molecular 193.25
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Fòrmula C14H11N
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Color Yellow to orange
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SMILES
C12=CC=CC=C1C=CC3=CC=CC=C3N2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
DMSO : 50 mg/mL (258.73 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 (protect from light). 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 (protect from light). 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 (12.94 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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 (282 KB)
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SDS (597 KB)
- English - EN (597 KB)
- Français - FR (597 KB)
- Deutsch - DE (597 KB)
- Norwegian - NO (597 KB)
- Español - ES (597 KB)
- Swedish - SV (597 KB)
- Italian - IT (597 KB)
- Korean - KR (597 KB)
- Portuguese - PT (597 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Christian P, et al. Crystallization of Carbamazepine in Proximity to Its Precursor Iminostilbene and a Silica Surface. Cryst Growth Des. 2016 May 4;16(5):2771-2778. Epub 2016 Mar 30. [Content Brief]
[2]. Lu S, et al. Iminostilbene, a novel small-molecule modulator of PKM2, suppresses macrophage inflammation in myocardial ischemia-reperfusion injury. J Adv Res. 2020 Sep 9;29:83-94. [Content Brief]
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 (protect from light). 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 | 5.1746 mL | 25.8732 mL | 51.7464 mL | 129.3661 mL |
| 5 mM | 1.0349 mL | 5.1746 mL | 10.3493 mL | 25.8732 mL | |
| 10 mM | 0.5175 mL | 2.5873 mL | 5.1746 mL | 12.9366 mL | |
| 15 mM | 0.3450 mL | 1.7249 mL | 3.4498 mL | 8.6244 mL | |
| 20 mM | 0.2587 mL | 1.2937 mL | 2.5873 mL | 6.4683 mL | |
| 25 mM | 0.2070 mL | 1.0349 mL | 2.0699 mL | 5.1746 mL | |
| 30 mM | 0.1725 mL | 0.8624 mL | 1.7249 mL | 4.3122 mL | |
| 40 mM | 0.1294 mL | 0.6468 mL | 1.2937 mL | 3.2342 mL | |
| 50 mM | 0.1035 mL | 0.5175 mL | 1.0349 mL | 2.5873 mL | |
| 60 mM | 0.0862 mL | 0.4312 mL | 0.8624 mL | 2.1561 mL | |
| 80 mM | 0.0647 mL | 0.3234 mL | 0.6468 mL | 1.6171 mL | |
| 100 mM | 0.0517 mL | 0.2587 mL | 0.5175 mL | 1.2937 mL |
Iminostilbene Related Classifications
HY-N7064 Related Classifications
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