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Gsk1016790a

CAS No.:
942206-85-1
Catalog Number:
AG00GUB4
Molecular Formula:
C28H32Cl2N4O6S2
Molecular Weight:
655.6129
Pack Size
Purity
Availability
Location
Price(USD)
Quantity
  
1mg
≥98%
1 week
United States
$91
- +
5mg
≥98%
1 week
United States
$153
- +
10mg
≥98%
1 week
United States
$214
- +
25mg
≥98%
1 week
United States
$361
- +
100mg
99%
1 week
United States
$1307
- +
Product Description
Catalog Number:
AG00GUB4
Chemical Name:
Gsk1016790a
CAS Number:
942206-85-1
Molecular Formula:
C28H32Cl2N4O6S2
Molecular Weight:
655.6129
MDL Number:
MFCD12912413
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
InChI Key:
IVYQPSHHYIAUFO-VXKWHMMOSA-N
SMILES:
OC[C@@H](C(=O)N1CCN(CC1)C(=O)[C@@H](NC(=O)c1cc2c(s1)cccc2)CC(C)C)NS(=O)(=O)c1ccc(cc1Cl)Cl
Properties
Complexity:
1070  
Compound Is Canonicalized:
Yes
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
2  
Defined Bond Stereocenter Count:
0
Exact Mass:
654.114g/mol
Formal Charge:
0
Heavy Atom Count:
42  
Hydrogen Bond Acceptor Count:
8  
Hydrogen Bond Donor Count:
3  
Isotope Atom Count:
0
Molecular Weight:
655.606g/mol
Monoisotopic Mass:
654.114g/mol
Rotatable Bond Count:
10  
Topological Polar Surface Area:
173A^2
Undefined Atom Stereocenter Count:
0
Undefined Bond Stereocenter Count:
0
XLogP3:
4.4  
Literature
Title Journal
Activation of TRPV3 by Wood Smoke Particles and Roles in Pneumotoxicity. Chemical research in toxicology 20180521
A novel TRPV4-specific agonist inhibits monocyte adhesion and atherosclerosis. Oncotarget 20160621
Identification of potent Yes1 kinase inhibitors using a library screening approach. Bioorganic & medicinal chemistry letters 20130801
Optical recording reveals novel properties of GSK1016790A-induced vanilloid transient receptor potential channel TRPV4 activity in primary human endothelial cells. Molecular pharmacology 20120901
TRPV4 in porcine lens epithelium regulates hemichannel-mediated ATP release and Na-K-ATPase activity. American journal of physiology. Cell physiology 20120615
Elementary Ca2+ signals through endothelial TRPV4 channels regulate vascular function. Science (New York, N.Y.) 20120504
Hypotonicity-induced TRPV4 function in renal collecting duct cells: modulation by progressive cross-talk with Ca2+-activated K+ channels. Cell calcium 20120201
Effects of TRPV4 cation channel activation on the primary bladder afferent activities of the rat. Neurourology and urodynamics 20120101
Characterization of transient receptor potential vanilloid channel 4 (TRPV4) in human corneal endothelial cells. Experimental eye research 20111101
Mutations in TRPV4 cause an inherited arthropathy of hands and feet. Nature genetics 20111002
Transient receptor potential vanilloid 4 (TRPV4)-dependent calcium influx and ATP release in mouse oesophageal keratinocytes. The Journal of physiology 20110715
The polymodal ion channel transient receptor potential vanilloid 4 modulates calcium flux, spiking rate, and apoptosis of mouse retinal ganglion cells. The Journal of neuroscience : the official journal of the Society for Neuroscience 20110511
Determinants of TRPV4 activity following selective activation by small molecule agonist GSK1016790A. PloS one 20110101
Inhibition of the cation channel TRPV4 improves bladder function in mice and rats with cyclophosphamide-induced cystitis. Proceedings of the National Academy of Sciences of the United States of America 20101102
Activation of Trpv4 reduces the hyperproliferative phenotype of cystic cholangiocytes from an animal model of ARPKD. Gastroenterology 20100701
TRPV4-mediated endothelial Ca2+ influx and vasodilation in response to shear stress. American journal of physiology. Heart and circulatory physiology 20100201
Functional TRPV4 channels and an absence of capsaicin-evoked currents in freshly-isolated, guinea-pig urothelial cells. Channels (Austin, Tex.) 20090101
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. The Journal of pharmacology and experimental therapeutics 20080801
Systemic activation of the transient receptor potential vanilloid subtype 4 channel causes endothelial failure and circulatory collapse: Part 2. The Journal of pharmacology and experimental therapeutics 20080801
Properties