917562-33-5 Usage
Uses
Used in Pharmaceutical and Biomedical Research:
JT010 is used as a potent and selective TRPA1 channel activator for studying the role of TRPA1 channels in various physiological and pathological processes. Its activation of the TRPA1 channel by covalently and site-selectively binding to Cys621 allows researchers to investigate the molecular mechanisms underlying TRPA1 channel function and its involvement in sensory perception, pain transmission, and other cellular responses.
Used in Drug Discovery and Development:
JT010 serves as a valuable lead compound for the development of new drugs targeting TRPA1 channels. Its high selectivity for TRPA1 over other TRP channels can be leveraged to design drugs with minimized off-target effects, potentially leading to safer and more effective therapeutic agents for treating conditions associated with TRPA1 channel dysregulation.
Used in Toxicological Studies:
Due to its potent and selective activation of TRPA1 channels, JT010 can be employed in toxicological studies to evaluate the potential adverse effects of TRPA1 channel activation. This can help in understanding the safety profile of TRPA1-targeting drugs and guide the development of safer therapeutic agents.
Used in Ion Channel Research:
JT010 is used as a research tool to investigate the structure, function, and regulation of TRPA1 channels. Its ability to selectively activate TRPA1 channels at low concentrations (EC50 = 65 nM) makes it an ideal probe for studying the molecular and biophysical properties of these channels, as well as their interactions with other cellular components and signaling pathways.
Biochem/physiol Actions
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).
Check Digit Verification of cas no
The CAS Registry Mumber 917562-33-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,1,7,5,6 and 2 respectively; the second part has 2 digits, 3 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 917562-33:
(8*9)+(7*1)+(6*7)+(5*5)+(4*6)+(3*2)+(2*3)+(1*3)=185
185 % 10 = 5
So 917562-33-5 is a valid CAS Registry Number.
917562-33-5Relevant academic research and scientific papers
Takaya, Junichiro,Mio, Kazuhiro,Shiraishi, Takuya,Kurokawa, Tatsuki,Otsuka, Shinya,Mori, Yasuo,Uesugi, Motonari
, p. 15859 - 15864 (2015)
TRPA1 is a member of the transient receptor potential (TRP) cation channel family that is expressed primarily on sensory neurons. This chemosensor is activated through covalent modification of multiple cysteine residues with a wide range of reactive compounds including allyl isothiocyanate (AITC), a spicy component of wasabi. The present study reports on potent and selective agonists of TRPA1, discovered through screening 1657 electrophilic molecules. In an effort to validate the mode of action of hit molecules, we noted a new TRPA1-selective agonist, JT010 (molecule 1), which opens the TRPA1 channel by covalently and site-selectively binding to Cys621 (EC50 = 0.65 nM). The results suggest that a single modification of Cys621 is sufficient to open the TRPA1 channel. The TRPA1-selective probe described herein might be useful for further mechanistic studies of TRPA1 activation.
