CBA (Compound 5; 4-Chloro-2-[[2-(2-chlorophenoxy)acetyl]amino]benzoic acid) is a cell penetrant, potent and selective TRPM4 (Transient receptor potential melastatin member 4) inhibitor that shows not significant activity against TRPM5, TRPM7, TRPM8, TRPV1, TRPV3, TRPV6. It rescues functional expression of mutant A432T TRPM4 in cells. CBA (Compound 5) exhibits neuroprotective activity against glutamate-induced neurodegeneration.
cell penetrant, potent and selective TRPM4 (Transient receptor potential melastatin member 4) inhibitor
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Transient receptor potential melastatin member 4 (TRPM4), a Ca2+-activated nonselective cation channel, has been found to mediate cell membrane depolarization in immune response, insulin secretion, cardiovascular diseases, and cancer. In murine experimental autoimmune encephalomyelitis (EAE), TRPM4 deletion and administration of
British journal of pharmacology, 175(12), 2504-2519 (2018-03-27)
TRPM4 is a calcium-activated non-selective cation channel expressed in many tissues and implicated in several diseases, and has not yet been validated as a therapeutic target due to the lack of potent and selective inhibitors. We sought to discover a
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