GSK1016790A

InvivoChem Cat #:V3576CAS #:942206-85-1 Purity >=98%

Description: GSK1016790A is a novel and potent transient receptor potential vanilloid 4 (TRPV4) activator. TRPV4 channel agonist GSK1016790A (GSK) caused concentration-dependent relaxation (Emax 86.9+/-4.6%; pD2 8.7+/-0.24) of the endothelium-intact rat pulmonary artery. Combined presence of apamin and TRAM-34 significantly attenuated the relaxation (Emax 61.1+/-6.0%) to GSK. l-NAME (100uM) significantly attenuated (8.2+/-2.9%) the relaxation response to GSK that was resistant to apamin plus TRAM-34. However, presence of ICI192605 or furegrelate alongwith l-NAME revealed the GSK-mediated EDHF-response (Emax of 28.5+/-5.2%; Emax 24.5+/-4.3%) in this vessel, respectively. Further, these two TxA2 modulators (ICI/furegrelate) alongwith l-NAME had no effect on SNP-induced endothelium-independent relaxation in comparison to l-NAME alone.

References: Pharmacol Rep, 2016 Jun, 68(3):620-6.; PLoS One, 2011 Feb 14; 6(2):e16713.

-20C for 3 years in powder form

Synonym: GSK1016790A; GSK-1016790A; GSK 1016790A.
Chemical Name: N-[(2S)-1-[4-[(2S)-2-[(2, 4-dichlorophenyl)sulfonylamino]-3-hydroxypropanoyl]piperazin-1-yl]-4-methyl-1-oxopentan-2-yl]-1-benzothiophene-2-carboxamide
InChi Key: IVYQPSHHYIAUFO-VXKWHMMOSA-N
InChi Code: 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
SMILES Code: O=C(C1=CC2=CC=CC=C2S1)N[CH](CC(C)C)C(N3CCN(C([CH](NS(=O)(C4=CC=C(Cl)C=C4Cl)=O)CO)=O)CC3)=O