GSK1016790A
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
GSK1016790A is a small molecule TRPV4 channel activator [1].
TRPV4 is a Ca2+-permeable, nonselective cation channel that has been involved in multiple physiologic functions, such as the regulation of systemic osmotic pressure, vascular function, skin barrier function, airway- and lung function, and in pain. The channel is activated by osmotic, mechanical, chemical cues and thermal changes. Channel activation can be sensitized by inflammation and injury. Mutations of TRPV4 may lead to premature osteoarthritis, skeletal dysplasias, and neurological motor function disorders [2].
In mouse and human TRPV4-expressing human embryonic kidney (HEK) cells, GSK1016790A elicited Ca2+ influx with the EC50 values of 18 and 2.1 nM, respectively. GSK1016790A dose-dependently evoked the activation of TRPV4 whole-cell currents at concentrations above 1 nM [1]. TRPV4 activation with GSK1016790A contracted TRPV4+/+ mouse bladders in vitro. Infusion of GSK1016790A into the bladders of TRPV4+/+ mice induced bladder overactivity with no effect in TRPV4-/- mice [1].
References:
[1] Thorneloe K S, Sulpizio A C, Lin Z, et al. 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[J]. Journal of Pharmacology and Experimental Therapeutics, 2008, 326(2): 432-442.
[2] Nilius B, Owsianik G, Voets T, et al. Transient receptor potential cation channels in disease[J]. Physiological reviews, 2007, 87(1): 165-217.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 655.6 |
Cas No. | 942206-85-1 |
Formula | C28H32Cl2N4O6S2 |
Solubility | ≥50.4 mg/mL in DMSO; ≥26.3 mg/mL in EtOH; insoluble in H2O |
Chemical Name | N-[(1S)-1-[[4-[(2S)-2-[[(2,4-dichlorophenyl)sulfonyl]amino]-3-hydroxy-1-oxopropyl]-1-piperazinyl]carbonyl]-3-methylbutyl]-benzo[b]thiophene-2-carboxamide |
SDF | Download SDF |
Canonical 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 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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