JT010 is a non-cytotoxic and highly stable (>90% remains after 2 h in 1 mM DTT or 2-mercaptoethanol) chloroacetamido warhead-carrying thiazole derivative that acts as a potent and TRPA1-selective channel activator via covalent modification of TRPA1 active site Cys621. JT0101 stimulates calcium influx in TRPA1-transfected HEK293 cells in a dose-dependent manner (EC50 = 650 pM) with excellent selectivity over TRPV1, TRPV3, TRPV4, TRPM2, TRPM8, and TRPC5 channels (EC50 >1 μM).
JT010 is a non-cytotoxic and highly stable chloroacetamido warhead-carrying thiazole derivative.
The American journal of pathology, 190(12), 2417-2426 (2020-09-14)
Increased expression of the transient receptor potential ankyrin 1 (TRPA1) channel has been detected in carious tooth pulp, suggesting involvement of TRPA1 in defense or repair of this tissue after exogenous noxious stimuli. This study aimed to elucidate the induction
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