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
PubChem CID
ChemSpider
ChEBI
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC28H32Cl2N4O6S2
Molar mass655.61 g·mol−1
3D model (JSmol)
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 (aka GSK101) 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

  1. ↑ Thorneloe KS, Sulpizio AC, Lin Z, Figueroa DJ, Clouse AK, McCafferty GP, et al. (August 2008). "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". The Journal of Pharmacology and Experimental Therapeutics. 326 (2): 432–42. doi:10.1124/jpet.108.139295. PMID 18499743. 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.
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