GSK1016790A CAS: 942206-85-1
MF: C28H32Cl2N4O6S2
MW: 655.61
A novel and potent TRPV4 channel agonist.

GSK1016790A (CAS 942206-85-1)

GSK1016790A | CAS 942206-85-1 is rated 5.0 out of 5 by 1.
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Alternate Names: (N-((1S)-1-{[4-((2S)-2-{[(2,4-Dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide
Application: GSK1016790A is a novel and potent TRPV4 channel agonist
CAS Number: 942206-85-1
Purity: ≥98%
Molecular Weight: 655.61
Molecular Formula: C28H32Cl2N4O6S2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data (including water content).

GSK1016790A is a novel and potent TRPV4 channel agonist. The TRPV4 (transient receptor potential vanilloid 4) member of the TRP superfamily has been implicated in numerous physiological processes. GSK1016790A elicited Ca2+ influx in mouse and human TRPV4 expressing HEK cells (EC50 values of 18 and 2.1 nM, respectively), and evoked a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM. It is 300 fold more potent than 4a-PDD.


References

1. Thorneloe, K.S., et al. 2008. J. Pharmacol. Exp. Ther. 326, 432-442. PMID: 18499743
2. Willette, R.N. et al. 2008. J. Pharmacol. Exp. Ther. 326(2): 443-452. PMID: 18499744
3. Thoppil, R.J. et al. 2015. Sci Rep. 5 : 14257. PMID: 26388427

Physical State :
Solid
Solubility :
Soluble in DMSO: >10 mg/mL
Storage :
Store at -20° C
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
23630211
SMILES :
CC(C)C[[email protected]@H](C(=O)N1CCN(CC1)C(=O)[[email protected]](CO)NS(=O)(=O)C2=C(C=C(C=C2)Cl)Cl)NC(=O)C3=CC4=CC=CC=C4S3

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Certificate of Analysis

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GSK1016790A (CAS 942206-85-1)  Product Citations

See how others have used GSK1016790A (CAS 942206-85-1). Click on the entry to view the PubMed entry .

Citations 1 to 6 of 6 total

PMID: # 27159616  Li, Y. et al. 2016. PLoS ONE. 11: e0155006.

PMID: # 24762817  Berrout, J. et al. 2014. PloS one. 9: e95149.

PMID: # 22298783  Berrout, J. et al. 2012. The Journal of biological chemistry. 287: 8782-91.

PMID: # 22204737  Jin, M. et al. 2012. Cell calcium. 51: 131-9.

PMID: # 30207167  Am. J. Physiol. Renal Physiol. 315: F1626-F1636.

PMID: # 31760763  Am. J. Physiol. Gastrointest. Liver Physiol.

Citations 1 to 6 of 6 total
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Rated 5 out of 5 by from Thoppil Thoppil, RJ. et al. (PubMed 26388427) reported that TRPV4 channel activation by GSK1016790A selectively inhibits tumor endothelial cell proliferation. -SCBT Publication Review
Date published: 2015-02-27
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