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
![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 Structure](CAS/20150408/GIF/942206-85-1.gif)
- CAS No.
- 942206-85-1
- Chemical Name:
- 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
- Synonyms
- GSK101;CS-2774;GSK1016790A;GSK1016790A(GSK101);GSK-1016790A;GSK 1016790A;GSK1016790A;GSK-1016790A;GSK 1016790A;N-((S)-1-(4-(((2,4-dichlorophenyl)sulfonyl)-L-seryl)piperazin-1-yl)-4-methyl-1-oxopentan-2-yl)benzo[b]thiophene-2-carboxamide;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;(N-((1S)-1-{[4-((2S)-2-{[(2,4-Dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide;Benzo[b]thiophene-2-carboxamide, N-[(1S)-1-[[4-[(2S)-2-[[(2,4-dichlorophenyl)sulfonyl]amino]-3-hydroxy-1-oxopropyl]-1-piperazinyl]carbonyl]-3-methylbutyl]-
- CBNumber:
- CB92676060
- Molecular Formula:
- C28H32Cl2N4O6S2
- Molecular Weight:
- 655.61
- MDL Number:
- MFCD12912413
- MOL File:
- 942206-85-1.mol
- MSDS File:
- SDS
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 Properties
| Melting point | >119°C (dec.) |
|---|---|
| Density | 1.426±0.06 g/cm3(Predicted) |
| storage temp. | -20°C |
| solubility | DMSO: >10mg/mL |
| form | white solid |
| pka | 8.29±0.50(Predicted) |
| color | White to Off-White |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months. |
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 price More Price(28)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | G0798 | GSK1016790A ≥98% (HPLC) | 942206-85-1 | 10mg | $281 | 2024-03-01 | Buy |
| Sigma-Aldrich | G0798 | GSK1016790A ≥98% (HPLC) | 942206-85-1 | 50mg | $1110 | 2024-03-01 | Buy |
| Cayman Chemical | 17289 | GSK1016790A ≥98% | 942206-85-1 | 1mg | $32 | 2024-03-01 | Buy |
| Cayman Chemical | 17289 | GSK1016790A ≥98% | 942206-85-1 | 5mg | $86 | 2024-03-01 | Buy |
| Cayman Chemical | 17289 | GSK1016790A ≥98% | 942206-85-1 | 10mg | $139 | 2024-03-01 | Buy |
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 Chemical Properties,Uses,Production
Description
GSK-1016790A (942206-85-1) is a novel and potent TRPV4 channel activator. GSK-1016790A induced 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 4α-PDD and is a valuable tool for investigating the role of TRPV4 in physiological processes.
Uses
GSK 1016790A is a transient receptor potential vanilloid 4 (TRPV4) agonist.
Uses
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
Definition
ChEBI: GSK1016790A is a tertiary carboxamide that is piperazine in which one of the amino groups has undergone condensation with the carboxy group of N-[(2,4-dichlorophenyl)sulfonyl]-L-serine, while the other has undergone condensation with the carboxy group of N-(1-benzothiophen-2-ylcarbonyl)-L-leucine. It is a cell-permeable, potent and selective agonist of the TRPV4 (transient receptor potential vanilloid 4) channel. It has a role as a TRPV4 agonist. It is a member of 1-benzothiophenes, a N-acylpiperazine, a sulfonamide, a dichlorobenzene, a tertiary carboxamide and an aromatic primary alcohol.
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).
storage
Store at -20°C
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
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 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| Creative Enzymes | 1-516-855-7709 | info@creative-enzymes.com | United States | 8748 | 58 |
| Alfa Chemistry | +1-5166625404 | Info@alfa-chemistry.com | United States | 21317 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| Hangzhou MolCore BioPharmatech Co.,Ltd. | +86-057181025280; +8617767106207 | sales@molcore.com | China | 49739 | 58 |
| Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3136 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8474 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
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 Spectrum
942206-85-1(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)Related Search:
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