Overview
- Wei, H. et al. (2010) Neuropharmacology 58, 578.
Alomone Labs Chembridge-5861528 inhibits Allyl isothiocyanate induced calcium signal in TRPA1 expressing cells.Dose-response curve for the inhibition of human TRPA1 expressing HEK-293 cells loaded with Calcium 5 dye for changes in intracellular Ca2+ measurements. Allyl isothiocyanate (100 µM)-induced calcium signal was inhibited by 5 µM Chembridge-5861528 (#C-235), with estimated IC50 of about 4 µM.
- Wei, H. et al. (2010) Neuropharmacology 58, 578.
- Benemei, S. et al. (2013) J. Headache Pain 14, 71.
Chembridge-5861528 (CHEM), a derivative of HC-030031 compound, is a potent and selective TRPA1 (TRP ankyrin 1) channel antagonist. TRPA1 channels play an important role in models of inflammatory and neuropathic pain and have the ability to detect pungent or irritant compounds.
Administration of Chembridge-5861528 attenuates diabetic hypersensitivity. It reduces hypersensitivity by suppressing the TRPA1 channel-mediated facilitation of transmitter release from central terminals of primary afferent nerve fibers1,2.
Blocking TRPA1 channels may help in migraine attack and can be used as a possible target for its treatment.
Evidence in several studies shows that TRPA1 antagonists could serve as novel therapeutic strategies for the treatment of chemotherapeutic-induced peripheral neuropathy2.
Chembridge-5861528 (#C-235) is a highly pure, synthetic, and biologically active compound.
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