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GSK-1016790A

Chemical Structure : GSK-1016790A

CAS No.: 942206-85-1

GSK-1016790A (GSK1016790A;GSK 1016790A)

Catalog No.: PC-45654Not For Human Use, Lab Use Only.

GSK-1016790A is a potent TRPV4 channel agonist, induces Ca2+ influx in HEK cells expressing human TRPV4 with EC50 of 2.1 nM.

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Biological Activity

GSK-1016790A is a potent TRPV4 channel agonist, induces Ca2+ influx in HEK cells expressing human TRPV4 with EC50 of 2.1 nM.
GSK-1016790A displays no effect on TRPM8 and TRPA1.
GSK-1016790A evokes a dose-dependent activation of TRPV4 whole-cell currents at >1 nM, 300-fold more potent than 4alpha-PDD.
GSK-1016790A induces urinary bladder contraction and hyperactivity in TRPV4+/+ mice.

Physicochemical Properties

M.Wt 655.613
Formula C28H32Cl2N4O6S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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Solubility

DMSO: ≥ 33 mg/mL

Chemical Name/SMILES

Benzo[b]thiophene-2-carboxamide, N-[(1S)-1-[[4-[(2S)-2-[[(2,4-dichlorophenyl)sulfonyl]amino]-3-hydroxy-1-oxopropyl]-1-piperazinyl]carbonyl]-3-methylbutyl]-

References

1. Thorneloe KS, et al. J Pharmacol Exp Ther. 2008 Aug;326(2):432-42.

2. Rajasekhar P, et al. J Biol Chem. 2015 Nov 27;290(48):29051-62.

3. Hong Z, et al. Mol Neurobiol. 2016 Jan;53(1):759-768.

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