Molecular structure of GSK1016790A, CAS Number: 942206-85-1
GSK1016790A (CAS 942206-85-1)
See product citations (6)
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.
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SDS & Certificate of Analysis
GSK1016790A possesses a unique chemical structure, characterized as a tertiary carboxamide. It is derived from piperazine, where one of the amino groups condenses with the carboxy group of N-[(2,4-dichlorophenyl)sulfonyl]-L-serine, while the other amino group condenses with the carboxy group of N-(1-benzothiophen-2-ylcarbonyl)-L-leucine. This compound serves as a potent and selective agonist of the TRPV4 channel, readily permeating cell membranes. It belongs to the class of 1-benzothiophenes and exhibits characteristics of an N-acylpiperazine, a sulfonamide, a dichlorobenzene, a tertiary carboxamide, and an aromatic primary alcohol.
GSK1016790A (CAS 942206-85-1) References
- N-((1S)-1-{[4-((2S)-2-{[(2,4-dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A), a novel and potent transient receptor potential vanilloid 4 channel agonist induces urinary bladder contraction and hyperactivity: Part I. | Thorneloe, KS., et al. 2008. J Pharmacol Exp Ther. 326: 432-42. PMID: 18499743
- Systemic activation of the transient receptor potential vanilloid subtype 4 channel causes endothelial failure and circulatory collapse: Part 2. | Willette, RN., et al. 2008. J Pharmacol Exp Ther. 326: 443-52. PMID: 18499744
- Determinants of TRPV4 activity following selective activation by small molecule agonist GSK1016790A. | Jin, M., et al. 2011. PLoS One. 6: e16713. PMID: 21339821
- Optical recording reveals novel properties of GSK1016790A-induced vanilloid transient receptor potential channel TRPV4 activity in primary human endothelial cells. | Sullivan, MN., et al. 2012. Mol Pharmacol. 82: 464-72. PMID: 22689561
- Analysis of responses to the TRPV4 agonist GSK1016790A in the pulmonary vascular bed of the intact-chest rat. | Pankey, EA., et al. 2014. Am J Physiol Heart Circ Physiol. 306: H33-40. PMID: 24186096
- TRPV4 channel activation selectively inhibits tumor endothelial cell proliferation. | Thoppil, RJ., et al. 2015. Sci Rep. 5: 14257. PMID: 26388427
- Activation of TRPV4 Regulates Respiration through Indirect Activation of Bronchopulmonary Sensory Neurons. | Gu, QD., et al. 2016. Front Physiol. 7: 65. PMID: 26973533
- NO synthase inhibition attenuates EDHF-mediated relaxation induced by TRPV4 channel agonist GSK1016790A in the rat pulmonary artery: Role of TxA2. | Addison, MP., et al. 2016. Pharmacol Rep. 68: 620-6. PMID: 26991376
- A novel TRPV4-specific agonist inhibits monocyte adhesion and atherosclerosis. | Xu, S., et al. 2016. Oncotarget. 7: 37622-37635. PMID: 27191895
- Enhanced Oxidative Stress Is Responsible for TRPV4-Induced Neurotoxicity. | Hong, Z., et al. 2016. Front Cell Neurosci. 10: 232. PMID: 27799895
- The TRPV4 Agonist GSK1016790A Regulates the Membrane Expression of TRPV4 Channels. | Baratchi, S., et al. 2019. Front Pharmacol. 10: 6. PMID: 30728775
- TRPV4-induced inflammatory response is involved in neuronal death in pilocarpine model of temporal lobe epilepsy in mice. | Wang, Z., et al. 2019. Cell Death Dis. 10: 386. PMID: 31097691
- Transient receptor potential vanilloid 4 agonist GSK1016790A improves neurological outcomes after intracerebral hemorrhage in mice. | Asao, Y., et al. 2020. Biochem Biophys Res Commun. 529: 590-595. PMID: 32736678
Inhibitor of:
GlyR α2.Activator of:
CaMKIIγ, Enzyme, Fibulin-1, Gα 11, Muted, TMEM63B, TRPV4, and VR1.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
GSK1016790A, 10 mg | sc-255193 | 10 mg | $260.00 |