GSK1016790A

• CAT Number: I005599
• CAS Number: 942206-85-1
• Molecular Formula: C28H32Cl2N4O6S2
• Molecular Weight: 655.61
• Purity: ≥95%
• Synonyms: GSK-1016790A; (N-((1S)-1-{[4-((2S)-2-{[(2,4-Dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide
• Target: Neuronal Signaling
• Solubility: DMSO ≥ 33 mg/mL
• Storage: Store at -20°C
• IUPAC 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: 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

GSK1016790A(CAT: I005599) is a potent and selective transient receptor potential vanilloid 4 (TRPV4) agonist. It effectively induces calcium influx in cells expressing TRPV4 channels, with EC₅₀ values of 18 nM in mouse and 2.1 nM in human TRPV4-expressing HEK cells. Activation of TRPV4 by GSK1016790A plays a significant role in modulating urinary bladder function and vascular endothelial tone regulation, making it a valuable tool in Neurology and Cardiovascular research. This compound is instrumental in exploring TRPV4-mediated pathways involved in mechanosensation, osmoregulation, and inflammatory responses, contributing to the development of treatments for related disorders.