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GSK1016790A

SIGMA/G0798 - ≥98% (HPLC)

Synonym: GSK101; (N-((1S)-1-{[4-((2S)-2-{[(2,4-Dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide

CAS Number: 942206-85-1
Empirical Formula (Hill Notation): C28H32Cl2N4O6S2
Molecular Weight: 655.61
MDL Number: MFCD12912413
Linear Formula: C28H32Cl2N4O6S2
Product Type: Chemical

Catalog Number PKG Qty. Price Quantity
45-G0798-10MG 10 mg
$310.00
1/EA
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45-G0798-50MG 50 mg
$1220.00
1/EA
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assay ≥98% (HPLC)
color white
form solid
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
InChI key IVYQPSHHYIAUFO-VXKWHMMOSA-N
originator GlaxoSmithKline
Quality Level 100 
SMILES string CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N3CCN(CC3)C(=O)[C@H](CO)NS(=O)(=O)c4ccc(Cl)cc4Cl
solubility DMSO: >10 mg/mL
storage temp. −20°C
Application: GSK1016790A has been used:
• to stimulate transient receptor potential vanilloid 4 (TRPV4)-mediated currents in Xenopus laevis oocytes
• to stimulate cells in Ca2+ level measurement in human retinal capillary endothelial cells (HRCECs)
• to study the role of TRPV4 channels in brain injury after intracerebral hemorrhage (ICH)
• to trigger the opening of TRPV4 channels in bovine nucleus pulposus cells or Hanks′ Balanced Salt Solution

Biochem/physiol Actions: GSK1016790A is a novel and potent TRPV4 channel agonist.
Biochem/physiol Actions: GSK1016790A is a novel and potent TRPV4 channel agonist. The TRPV4 (transient receptor potential vanilloid 4) member of the TRP superfamily has been implicated in numerous physiological processes. GSK1016790A elicited Ca2+ influx in mouse and human TRPV4 expressing HEK cells (EC50 values of 18 and 2.1 nM, respectively), and evoked a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM. It is 300 fold more potent than 4a-PDD (Cat. No. P8014).
Features and Benefits: This compound was developed by GlaxoSmithKline . To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here .
Packaging: 10, 50 mg in glass bottle
RIDADR NONH for all modes of transport
WGK Germany WGK 1
Flash Point(F) Not applicable
Flash Point(C) Not applicable
Purity ≥98% (HPLC)
Storage Temp. −20°C
UNSPSC 12352200

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