TRPM4-IN-1
Based on 1 Customer Validation
TRPM4-IN-1 (CBA) is a potent and selective inhibitor of the cation channel TRPM4, with an IC50 of 1.5 μM. TRPM4-IN-1 can be used for the research of cardiac diseases and prostate cancer.
For research use only. We do not sell to patients.
- Purity: 99.17%
- CAS No.: 351424-20-9
- Formula: C15H11Cl2NO4
- Molecular Weight:340.16
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Membrane Transporter/Ion Channel Compound Library
HY-L011
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Neuronal Signaling Compound Library
HY-L013
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Anti-Cancer Compound Library
HY-L025
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Anti-Cardiovascular Disease Compound Library
HY-L046
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Mechanoreceptors Compound Library
HY-L095
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Anti-Prostate Cancer Compound Library
HY-L124
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Pain-Related Compound Library
HY-L139
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Membrane Protein-targeted Compound Library
HY-L149
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Membrane Receptor-targeted Compound Library
HY-L150
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Highly Selective Inhibitors Library
HY-L158
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Ion Channel Compound Library
HY-L166
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
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High-Throughput Bioactive Compound Library
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Biological Activity
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
1.5 μM
Compound: CBA
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Inhibition of Flag-tagged TRPM4 (unknown origin) expressed in HEK293 cells assessed as reduction in intracellular Na+ influx after 45 mins by ANG2 dye-based fluorescence assay
Inhibition of Flag-tagged TRPM4 (unknown origin) expressed in HEK293 cells assessed as reduction in intracellular Na+ influx after 45 mins by ANG2 dye-based fluorescence assay
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[PMID: 30708257] |
TRPM4-IN-1 (compound 5) is a potent and selective inhibitor of TRPM4 current in TRPM4 overexpressed HEK293 cells[1].
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TRPM4-IN-1 reversibly blocks endogenous TRPM4 currents in LNCaP (prostate cancer) cells[1].
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TRPM4-IN-1 (50 μM; Overnight) restores functional expression of A432T, a loss‐of‐expression TRPM4 variant[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells
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Concentration:50 μM
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Incubation Time:Overnight
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Result:Partial rescued the total and surface expression of A432T.
Chemical Information
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CAS No. 351424-20-9
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Appearance Solid
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Molecular Weight 340.16
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Formula C15H11Cl2NO4
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Color White to yellow
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SMILES
O=C(O)C1=CC=C(Cl)C=C1NC(COC2=CC=CC=C2Cl)=O
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Synonyms
CBA
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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
DMSO : 83.33 mg/mL (244.97 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.
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.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Lijo Cherian Ozhathil, et al. Identification of potent and selective small molecule inhibitors of the cation channel TRPM4. Br J Pharmacol. 2018 Jun; 175(12): 2504–2519. [Content Brief]
[2]. Clémence Delalande, et al. Optimizing TRPM4 inhibitors in the MHFP6 chemical space. Eur J Med Chem. 2019 Mar 15;166:167-177. [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. 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 | 2.9398 mL | 14.6990 mL | 29.3979 mL | 73.4948 mL |
| 5 mM | 0.5880 mL | 2.9398 mL | 5.8796 mL | 14.6990 mL | |
| 10 mM | 0.2940 mL | 1.4699 mL | 2.9398 mL | 7.3495 mL | |
| 15 mM | 0.1960 mL | 0.9799 mL | 1.9599 mL | 4.8997 mL | |
| 20 mM | 0.1470 mL | 0.7349 mL | 1.4699 mL | 3.6747 mL | |
| 25 mM | 0.1176 mL | 0.5880 mL | 1.1759 mL | 2.9398 mL | |
| 30 mM | 0.0980 mL | 0.4900 mL | 0.9799 mL | 2.4498 mL | |
| 40 mM | 0.0735 mL | 0.3675 mL | 0.7349 mL | 1.8374 mL | |
| 50 mM | 0.0588 mL | 0.2940 mL | 0.5880 mL | 1.4699 mL | |
| 60 mM | 0.0490 mL | 0.2450 mL | 0.4900 mL | 1.2249 mL | |
| 80 mM | 0.0367 mL | 0.1837 mL | 0.3675 mL | 0.9187 mL | |
| 100 mM | 0.0294 mL | 0.1470 mL | 0.2940 mL | 0.7349 mL |
TRPM4-IN-1 Related Classifications
HY-122605 Related Classifications
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