1649479-05-9
Chemical Structure
GRC-17536
- CAS No.: 1649479-05-9
- Formula:C20H13F5KN4O3S2
- Molecular Weight:555.56
IUPAC Name: N-(4-(2,4-difluoro-3-(trifluoromethyl)phenyl)thiazol-2-yl)-2-(1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-5-yl)acetamide, potassium salt
InChIKey: ZROMZAGVBVNUBJ-UHFFFAOYSA-N
SMILES: [K].O=C1C2=C(SC=C2CC(=O)NC3=NC(=CS3)C=4C=CC(F)=C(C4F)C(F)(F)F)N(C(=O)N1C)C
Biological Activity: GRC-17536 is a TRPA1 antagonist with selective inhibition of TRPA1-mediated calcium influx[1][2][3][4].GRC-17536 binds to TRPA1 binding site 2 to inhibit channel activity[3].GRC-17536 reduces irritant-induced cough responses and citric acid-induced cough responses[2][4].GRC-17536 exhibits antitussive activity[1][4].GRC-17536 has poor pharmacokinetic and bioavailability properties, leading to discontinued development after a Phase IIa study[1][2].GRC-17536 can be used for the research of painful diabetic polyneuropathy, peripheral diabetic neuropathy, asthma, and chronic cough[1][2][3][4].
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GRC-17536 | GRC-17536 is a TRPA1 antagonist with selective inhibition of TRPA1-mediated calcium influx.GRC-17536 binds to TRPA1 binding site 2 to inhibit channel activity.GRC-17536 reduces irritant-induced cough responses and citric acid-induced cough responses.GRC-17536 exhibits antitussive activity.GRC-17536 has poor pharmacokinetic and bioavailability properties, leading to discontinued development after a Phase IIa study.GRC-17536 can be used for the research of painful diabetic polyneuropathy, peripheral diabetic neuropathy, asthma, and chronic cough. | |||||||||||||||||||||
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- [1]. Anand S, et al. A Comprehensive Review on the Regulatory Action of TRP Channels: A Potential Therapeutic Target for Nociceptive Pain. Neuroscience insights. 2023;18:26331055231220340.
- [2]. Chen H, et al. Transient receptor potential ankyrin 1 (TRPA1) antagonists: a patent review (2015-2019). Expert opinion on therapeutic patents. 2020 Sep;30(9):643-657. [Content Brief]
- [3]. Mesch S, et al. Discovery of , a Selective CNS Penetrant Chemical Probe as Transient Receptor Potential Ankyrin 1 (TRPA1) Antagonist. Journal of medicinal chemistry. 2023 Jan 26;66(2):1583-1600.
- [4]. Mukhopadhyay I, et al. Transient receptor potential ankyrin 1 receptor activation in vitro and in vivo by pro-tussive agents: GRC 17536 as a promising anti-tussive therapeutic. PloS one. 2014;9(5):e97005.
Keywords
