GSK1016790A

• CAT Number: I005599
• CAS Number: 942206-85-1
• Molecular Formula: C28H32Cl2N4O6S2
• Molecular Weight: 655.6
• Purity: ≥95%
• Target: TRP Channel
• Solubility: DMSO ≥ 33 mg/mL
• Storage: Store at -20°C
• 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
• InChIKey: IVYQPSHHYIAUFO-VXKWHMMOSA-N
• SMILES: ClC1=CC=C(S(N[C@H](C(N2CCN(C([C@@H](NC(C3=CC4=C(C=CC=C4)S3)=O)CC(C)C)=O)CC2)=O)CO)(=O)=O)C(Cl)=C1

Transient receptor potential vanilloid 4 (TRPV4) is a nonselective cation channel thought to be involved in osmoregulation, hyperalgesia, and control of epithelial cell volume.
GSK1016790A is a TRPV4 agonist that has been reported to elicit calcium influx in HEK cells expressing mouse or human TRPV4 (EC50s = 18 and 2.1 nM, respectively). It has been used to demonstrate a role for TRPV4 in regulating urinary bladder activity and endothelial control of vascular tone.

Reference

1:NO synthase inhibition attenuates EDHF-mediated relaxation induced by TRPV4 channel agonist GSK1016790A in the rat pulmonary artery: Role of TxA2. Addison MP, Singh TU, Parida S, Choudhury S, Kasa JK, Sukumaran SV, Darzi SA, Kandasamy K, Singh V, Kumar D, Mishra SK.Pharmacol Rep. 2016 Jun;68(3):620-6. doi: 10.1016/j.pharep.2016.01.003. Epub 2016 Jan 19. PMID: 26991376 2:Analysis of responses to the TRPV4 agonist GSK1016790A in the pulmonary vascular bed of the intact-chest rat. Pankey EA, Zsombok A, Lasker GF, Kadowitz PJ.Am J Physiol Heart Circ Physiol. 2014 Jan 1;306(1):H33-40. doi: 10.1152/ajpheart.00303.2013. Epub 2013 Nov 1. PMID: 24186096 Free PMC Article3:Optical recording reveals novel properties of GSK1016790A-induced vanilloid transient receptor potential channel TRPV4 activity in primary human endothelial cells. Sullivan MN, Francis M, Pitts NL, Taylor MS, Earley S.Mol Pharmacol. 2012 Sep;82(3):464-72. doi: 10.1124/mol.112.078584. Epub 2012 Jun 11. PMID: 22689561 Free PMC Article4:Determinants of TRPV4 activity following selective activation by small molecule agonist GSK1016790A. Jin M, Wu Z, Chen L, Jaimes J, Collins D, Walters ET, O/’Neil RG.PLoS One. 2011 Feb 14;6(2):e16713. doi: 10.1371/journal.pone.0016713. PMID: 21339821 Free PMC Article5: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, 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.J Pharmacol Exp Ther. 2008 Aug;326(2):432-42. doi: 10.1124/jpet.108.139295. Epub 2008 May 22. Erratum in: J Pharmacol Exp Ther. 2011 Jul;338(1):410. PMID: 18499743 Free Article