GSK1016790A - CAS 942206-85-1
Catalog number: B0084-382782
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C28H32Cl2N4O6S2
Molecular Weight:
655.61
COA:
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Targets:
TRP Channel
Description:
GSK1016790A is a novel and potent transient receptor potential vanilloid 4 (TRPV4) agonist. It has been used to demonstrate a role for TRPV4 in regulating urinary bladder activity and endothelial control of vascular tone. It elicited Ca2+ influx in mouse and human TRPV4 expressing HEK cells with EC50 values of 18 and 2.1 nM, respectively. It also evoked a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM, which is 300 fold more potent than 4a-PDD. It was developed by GlaxoSmithKline.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-382782 100 mg $748 In stock
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Purity:
>98 %
Appearance:
White Solid
Synonyms:
N-((S)-1-(4-((S)-2-(2,4-dichlorophenylsulfonaMido)-3-hydroxypropanoyl)piperazin-1-yl)-4-Methyl-1-oxopentan-2-yl)benzo[b]thiophene-2-carboxaMide;GSK-1016790A
Solubility:
DMSO ≥ 33 mg/mL
Storage:
-20°C Freezer
MSDS:
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Application:
GSK1016790A regulats urinary bladder activity and endothelial control of vascular tone.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
Density:
1.426±0.06 g/cm3 | Condition: Temp: 20 °C Press: 760 Tor
InChIKey:
IVYQPSHHYIAUFO-VXKWHMMOSA-N
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
Canonical SMILES:
CC(C)CC(C(=O)N1CCN(CC1)C(=O)C(CO)NS(=O)(=O)C2=C(C=C(C=C2)Cl)Cl)NC(=O)C3=CC4=CC=CC=C4S3
Current Developer:
GSK1016790A was developed by GlaxoSmithKline.
1.NO synthase inhibition attenuates EDHF-mediated relaxation induced by TRPV4 channel agonist GSK1016790A in the rat pulmonary artery: Role of TxA2.
Addison MP1, Singh TU2, Parida S1, Choudhury S1, Kasa JK1, Sukumaran SV1, Darzi SA1, Kandasamy K1, Singh V1, Kumar D1, Mishra SK1. Pharmacol Rep. 2016 Jun;68(3):620-6. doi: 10.1016/j.pharep.2016.01.003. Epub 2016 Jan 19.
BACKGROUND: The aim of the present study was to observe the concomitant activation of nitric oxide (NO) and endothelium-derived hyperpolarizing factor (EDHF) pathways by TRPV4 channel agonist GSK1016790A in the rat pulmonary artery and explore the mechanism by which NO synthase inhibition attenuates EDHF-mediated relaxation in endothelium-intact rat pulmonary artery.
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CAS 942206-85-1 GSK1016790A

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