GSK1016790A

GSK1016790A
Identifiers
	IUPAC name N-[(1S)-1-[[4-[(2S)-2-[[(2,4-Dichlorophenyl)sulfonyl]amino]-3-hydroxy-1-oxopropyl]-1-piperazinyl]carbonyl]-3-methylbutyl]benzo[b]thiophene-2-carboxamide;
CAS Number	942206-85-1;
PubChem CID	23630211;
ChemSpider	29310491;
ChEBI	CHEBI:140524;
CompTox Dashboard (EPA)	DTXSID30635248 ;
Chemical and physical data
Formula	C28H32Cl2N4O6S2
Molar mass	655.61 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC(C)C[C@H](NC(C1=CC2=CC=CC=C2S1)=O)C(N3CCN(CC3)C([C@H](CO)NS(=O)(C4=C(Cl)C=C(Cl)C=C4)=O)=O)=O;
	InChI InChI=1S/C28H32Cl2N4O6S2/c1-17(2)13-21(31-26(36)24-14-18-5-3-4-6-23(18)41-24)27(37)33-9-11-34(12-10-33)28(38)22(16-35)32-42(39,40)25-8-7-19(29)15-20(25)30/h3-8,14-15,17,21-22,32,35H,9-13,16H2,1-2H3,(H,31,36)/t21-,22-/m0/s1; Key:IVYQPSHHYIAUFO-VXKWHMMOSA-N;

GSK1016790A is a drug developed by GlaxoSmithKline which acts as a potent and selective agonist for the TRPV4 receptor. It has been used to study the role of TRPV4 receptors in the function of smooth muscle tissue, particularly that lining blood vessels, lymphatic system and the bladder.[1][2][3][4][5]

References

{{cite journal | vauthors = Thorneloe KS, Sulpizio AC, Lin Z, Figueroa DJ, Clouse AK, McCafferty GP, Chendrimada TP, Lashinger ES, Gordon E, Evans L, Misajet BA, Demarini DJ, Nation JH, Casillas LN, Marquis RW, Votta BJ, Sheardown SA, Xu X, Brooks DP, Laping NJ, Westfall TD | display-authors = 6 | title = 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 | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 326 | issue = 2 | pages = 432–42 | date = August 2008 | pmid = 18499743 | doi = 10.1124/jpet.108.139295 | s2cid = 517735 }}
Vincent F, Duncton MA (2011). "TRPV4 agonists and antagonists". Current Topics in Medicinal Chemistry. 11 (17): 2216–26. doi:10.2174/156802611796904861. PMID 21671873.
Xu S (May 2020). "Therapeutic potential of blood flow mimetic compounds in preventing endothelial dysfunction and atherosclerosis". Pharmacological Research. 155: 104737. doi:10.1016/j.phrs.2020.104737. PMID 32126273.
Thapak P, Vaidya B, Joshi HC, Singh JN, Sharma SS (September 2020). "Therapeutic potential of pharmacological agents targeting TRP channels in CNS disorders". Pharmacological Research. 159: 105026. doi:10.1016/j.phrs.2020.105026. PMID 32562815.
Solari E, Marcozzi C, Bistoletti M, Baj A, Giaroni C, Negrini D, Moriondo A (August 2020). "TRPV4 channels' dominant role in the temperature modulation of intrinsic contractility and lymph flow of rat diaphragmatic lymphatics". American Journal of Physiology. Heart and Circulatory Physiology. 319 (2): H507–H518. doi:10.1152/ajpheart.00175.2020. PMID 32706268.

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[1] {{cite journal | vauthors = Thorneloe KS, Sulpizio AC, Lin Z, Figueroa DJ, Clouse AK, McCafferty GP, Chendrimada TP, Lashinger ES, Gordon E, Evans L, Misajet BA, Demarini DJ, Nation JH, Casillas LN, Marquis RW, Votta BJ, Sheardown SA, Xu X, Brooks DP, Laping NJ, Westfall TD | display-authors = 6 | title = 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 | journal = The Journal of Pharmacology and Experimental Therapeutics | volume = 326 | issue = 2 | pages = 432–42 | date = August 2008 | pmid = 18499743 | doi = 10.1124/jpet.108.139295 | s2cid = 517735 }}

[2] Vincent F, Duncton MA (2011). "TRPV4 agonists and antagonists". Current Topics in Medicinal Chemistry. 11 (17): 2216–26. doi:10.2174/156802611796904861. PMID 21671873.

[3] Xu S (May 2020). "Therapeutic potential of blood flow mimetic compounds in preventing endothelial dysfunction and atherosclerosis". Pharmacological Research. 155: 104737. doi:10.1016/j.phrs.2020.104737. PMID 32126273.

[4] Thapak P, Vaidya B, Joshi HC, Singh JN, Sharma SS (September 2020). "Therapeutic potential of pharmacological agents targeting TRP channels in CNS disorders". Pharmacological Research. 159: 105026. doi:10.1016/j.phrs.2020.105026. PMID 32562815.

[5] Solari E, Marcozzi C, Bistoletti M, Baj A, Giaroni C, Negrini D, Moriondo A (August 2020). "TRPV4 channels' dominant role in the temperature modulation of intrinsic contractility and lymph flow of rat diaphragmatic lymphatics". American Journal of Physiology. Heart and Circulatory Physiology. 319 (2): H507–H518. doi:10.1152/ajpheart.00175.2020. PMID 32706268.