GNE551 | TRPA1 agonist | Probechem Biochemicals

Chemical Structure : GNE551

CAS No.: 866347-75-3

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GNE551 (GNE-551)

货号: PC-38809Not For Human Use, Lab Use Only.

GNE551 is a potent, selective, non-covalent agonist of TRPA1 ion channel with EC50 of 254 nM in Ca2+ influx assays.

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生物&药学活性

GNE551 is a potent, selective, non-covalent agonist of TRPA1 ion channel with EC50 of 254 nM in Ca2+ influx assays.
GNE551 (1 μM) evoked outward currents at +80 mV and inward currents at −80 mV in whole-cell recordings assays, and evoked robust currents in TRPA1-expressing cells at 80 mV with EC50 of 141 nM, which could be blocked by 1 uM A-967079.
GNE551 (20 μM) did not activate or block human TRPV1, TRPM8, or TRPC6, did not inhibit human potassium channel hERG1 and sodium channels (hNav1.2., hNav1.5, or hNav1.7) at 10 μM.
GNE551 binds to a transmembrane pocket conserved in several other TRP channels.
Compared to the canonical covalent agonist AITC, GNE551 exhibits remarkable differences in channel modulation, pain response, and sensitivity to inhibitor treatment.

物理化学性质&存储条件

分子量	450.268
分子式	C18H17BrFN5O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	5-amino-1-(4-bromo-2-fluorobenzyl)-N-(2,5-dimethoxyphenyl)-1H-1,2,3-triazole-4-carboxamide

参考文献

1. Liu C,, et al. Neuron. 2021 Jan 20;109(2):273-284.e4.

GNE551 (GNE-551)

生物&药学活性

物理化学性质&存储条件

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GNE551 (GNE-551)

生物&药学活性

物理化学性质&存储条件

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