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TRPM4-IN-2 (Synonyms: NBA)

Katalog-Nr.GC68002 Copy One-Click Copy Product Info

TRPM4-IN-2 is a potent transient receptor potential melastatin 4 (TRPM4) inhibitor with an IC50 value of 0.16μM.

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TRPM4-IN-2 Chemische Struktur

Cas No.: 667411-04-3

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10mM (in 1mL DMSO)
132,00 $
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1mg
55,00 $
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5mg
120,00 $
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10mg
200,00 $
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25mg
440,00 $
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Sample solution is provided at 25 µL, 10mM.



Description of TRPM4-IN-2

TRPM4-IN-2 is a potent transient receptor potential melastatin 4 (TRPM4) inhibitor with an IC50 value of 0.16μM [1]. TRPM4-IN-2 binds in a pocket formed between the S3, S4, and TRP helices and the S4-S5 linker of TRPM4 to block the TRPM4 channel [2]. TRPM4-IN-2 has been widely used to decrease mouse TRPM4 currents and suppress arrhythmias [3].

In vitro, TRPM4-IN-2 treatment (100μM) for 48 hours significantly inhibited the proliferation of MDA-MB-231, A549 and KYSE30 cells [4]. Pre-treatment of HT22 cells with 10μM TRPM4-IN-2 for 2 hours significantly protected the cells from 5mM glutamate-induced cell death and disruption of cell integrity[5].

References:
[1] Stokłosa P, Borgström A, Hauert B, et al. Investigation of novel small molecular TRPM4 inhibitors in colorectal cancer cells[J]. Cancers, 2021, 13(21): 5400.
[2] Ekundayo B, Arullampalam P, Gerber C E, et al. Identification of a binding site for small molecule inhibitors targeting human TRPM4[J]. Nature communications, 2025, 16(1): 833.
[3] Hu Y, Cang J, Hiraishi K, et al. The role of TRPM4 in cardiac electrophysiology and arrhythmogenesis[J]. International Journal of Molecular Sciences, 2023, 24(14): 11798.
[4] Chang W, Gao W, Luo B, et al. Comprehensive insights into the role of TRPM4 in Pan-cancer progression and immune regulation[J]. ImmunoTargets and Therapy, 2025: 831-848.
[5] Bianchi B, Smith P A, Abriel H. The ion channel TRPM4 in murine experimental autoimmune encephalomyelitis and in a model of glutamate-induced neuronal degeneration[J]. Molecular brain, 2018, 11(1): 41.

Protocol of TRPM4-IN-2

Cell experiment [1]:

Cell lines

MDA-MB-231 cells

Preparation Method

MDA-MB-231 cells were cultivated in 96-well plate at a density of 5×103 cells/well in DMEM medium supplemented with 10% fetal bovine serum (FBS), and 1% penicillin/streptomycin. Cells were treated with different concentrations of the TRPM4-IN-2 (0, 0.1, 1, 10, 50, and 100µM) for 48h. The viability was determined.

Reaction Conditions

0, 0.1, 1, 10, 50, and 100µM; 48h

Applications

TRPM4-IN-2 treatment reduced the viability of MDA-MB-231 cells in a dose-dependent manner.

References:
[1] Chang W, Gao W, Luo B, et al. Comprehensive insights into the role of TRPM4 in Pan-cancer progression and immune regulation[J]. ImmunoTargets and Therapy, 2025: 831-848.

Chemical Properties of TRPM4-IN-2

Cas No. 667411-04-3 SDF
Überlieferungen NBA
Formula C19H14ClNO4 M.Wt 355.77
Löslichkeit 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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of TRPM4-IN-2

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.8108 mL 14.054 mL 28.108 mL
5 mM 562.2 μL 2.8108 mL 5.6216 mL
10 mM 281.1 μL 1.4054 mL 2.8108 mL
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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 saline, mix and clarify.

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3. All of the above co-solvents are available for purchase on the GlpBio website.

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