trpm4

TRPM4-IN-2 (NBA), also known as NBA, is a highly effective inhibitor of transient receptor potential melastatin 4 (TRPM4). Its inhibitory potency is represented by an IC 50 value of 0.16 μM. This compound serves as a valuable tool in the investigation of prostate cancer and colorectal cancer [1] [2].

NMDAR TRPM4-IN-2 is a potent interfacial inhibitor of NMDAR TRPM4 interaction.NMDAR TRPM4-IN-2 protects against MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss in mice.NMDAR TRPM4-IN-2 has neuroprotective activity against NMDA-induced hippocampal neuronal cell death and mitochondrial dysfunction. NMDAR TRPM4-IN-2 showed neuroprotective activity against NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons with an IC50 value of 2.1 μM.

TRPM4 inhibitor 8 is an inhibitor of Transient receptor potential melastatin 4(TRPM4) which contributes to viability, migration, cell cycle shift, and adhesion.

TRPM4-IN-1 (4-chloro-2-(2-(2-chlorophenoxy)acetamido)benzoic acid) is a potent and selective inhibitor of TRPM4 with an IC50 of 1.5 μM.

CMP233 is a potent antagonist of TRPM4, with an IC50 of 0.15 μM. It plays a significant role in the research of neurodegenerative diseases.

9-Phenanthrol is inhibitor of the transient receptor potential melastatin 4 (TRPM) channel, a Ca2+ -activated non-selective cation channel.

CIM0216 is a synthetic TRPM3 activator whose potency and apparent affinity greatly exceeds that of the canonical TRPM3 agonist.

HZS60 is a brain-penetrant NMDAR TRPM4 inhibitor that shows promise in ameliorating cerebral ischemia. It provides significant neuroprotection against ischemic injury in primary neurons caused by NMDA and oxygen-glucose deprivation reoxygenation. HZS60 demonstrates favorable pharmacokinetic properties and can inhibit cerebral ischemia-reperfusion injury, positioning it as a potential inhibitor for ischemic stroke.

ErSO-TFPy activates the sodium ion channel TRPM4, resulting in an imbalance of intracellular calcium and sodium ions. It exhibits low nanomolar-level cytotoxicity (IC50 = 5-25 nM) by inducing necrosis in ERα+ breast cancer cell lines. Additionally, ErSO-TFPy shows antitumor activity in mouse models.