942206-85-1 Usage
Description
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, also known as GSK-1016790A, is a novel and potent TRPV4 channel activator. It is characterized by its ability to induce Ca2+ influx in mouse and human TRPV4 expressing HEK cells with high potency, and evoke a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM. GSK-1016790A is 300-fold more potent than 4α-PDD, making it a valuable tool for investigating the role of TRPV4 in physiological processes.
Uses
Used in Pharmaceutical Research:
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 is used as a TRPV4 agonist for stimulating transient receptor potential vanilloid 4 (TRPV4)-mediated currents in Xenopus laevis oocytes. This application aids in understanding the underlying mechanisms of TRPV4 channel activation and its role in various physiological processes.
Used in Cellular Studies:
In human retinal capillary endothelial cells (HRCECs), 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 is used to stimulate cells in Ca2+ level measurement. This helps researchers to evaluate the effects of TRPV4 activation on intracellular calcium levels and its potential implications in various cellular functions.
Used in Neurological Research:
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 is utilized to study the role of TRPV4 channels in brain injury after intracerebral hemorrhage (ICH). This application is crucial for exploring the potential therapeutic effects of TRPV4 activation in the context of neurological disorders and injuries.
Used in Orthopedic Research:
In bovine nucleus pulposus cells, 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 is used to trigger the opening of TRPV4 channels. This research is important for understanding the role of TRPV4 channels in the intervertebral disc and its potential as a target for treating related conditions.
Overall, 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, or GSK-1016790A, is a versatile compound with applications in various research fields, including pharmaceutical, cellular, neurological, and orthopedic studies, due to its potent TRPV4 channel activating properties.
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).
References
1) Thorneloe et al. (2008), 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. Pharmacol. Exp. Ther., 326 432
Check Digit Verification of cas no
The CAS Registry Mumber 942206-85-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,4,2,2,0 and 6 respectively; the second part has 2 digits, 8 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 942206-85:
(8*9)+(7*4)+(6*2)+(5*2)+(4*0)+(3*6)+(2*8)+(1*5)=161
161 % 10 = 1
So 942206-85-1 is a valid CAS Registry Number.
