GSK205
Based on 13 publication(s) in Google Scholar
GSK205 is a potent, selective TRPV4 antagonist with an IC50 of 4.19 μM for inhibiting TRPV4-mediated Ca2+ influx.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.47%
- CAS 番号: 1263068-83-2
- 分子式: C24H25BrN4S
- 分子量:481.45
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 GSK205
More- Nat Commun. 2025 Sep 29;16(1):8541. [Abstract]
- J Clin Invest. 2024 May 21:e175057. [Abstract]
- Biomater Res. 2025 Apr 9:29:0182. [Abstract]
- Biofabrication. 2026 Feb 5;18(1). [Abstract]
- Cell Rep. 2025 Sep 22;44(10):116308. [Abstract]
- ACS Appl Bio Mater. 2021 Mar 15;4(3):2601-2613. [Abstract]
- Exp Cell Res. 2025 Apr 1;447(1):114515. [Abstract]
- Front Physiol. 2021 Dec 24;12:783891. [Abstract]
- bioRxiv. 2025 Oct 24.
- Drexel University. 2025.
- bioRxiv. 2025 Jun 15.
- bioRxiv. 2024 November 26.
- bioRxiv. 2023 May 26:2023.05.26.542500. [Abstract]
Customer Validation & Images
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Bio/Physico-chemical Assay
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WB
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Cell Imaging/Staining
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RT-PCR
生物活性
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TRPV4 21 μM (EC50) |
TRPV1 28 μM (EC50) |
GSK205 (100 μM) potently antagonizes TRPV4 in 3T3-F442A adipocytes, as it effectively blocks the calcium influx caused by TRPV4 agonist[1].
GSK205 (5 μM; 4 days; T3-F442A adipocytes) treatment results in increases expression of thermogenic genes (Mcp1, Mip1α, Mcp3, Rantes and Vcam, et al.) and is also accompanied by a decrease in the proinflammatory gene program. This shift resembles the gene expression changes seen in TRPV4-deficient adipocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:T3-F442A adipocytes
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Concentration:5 μM
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Incubation Time:4 days
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Result:Resulted in increased expression of thermogenic genes and is also accompanied by a decrease in the proinflammatory gene program.
GSK205 has a relatively short half-life of 2 hours in the plasma and adipose tissues[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6J mice with high-fat diet[1]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection; twice daily; for 7 days
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Result:Caused a reduced expression of the proinflammatory chemokines, macrophage marker and Tnfa in the EPI fat. Significantly improved glucose tolerance in diet-induced obese (DIO) mice.
化学情報
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CAS 番号 1263068-83-2
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性状 Solid
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分子量 481.45
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分子式 C24H25BrN4S
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Color Light yellow to yellow
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SMILES
CN(CCC1=CC=C(NC2=NC=C(C3=CC=CN=C3)S2)C=C1)CC4=CC=CC=C4.[H]Br
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (13)
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Journal Impact Factor
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Most Recent
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Nat Commun
Biomimetic organo-hydrogels reveal the adipose tissue local mechanical anisotropy regulates ovarian cancer invasion. [Abstract]2025 Sep 29;16(1):8541. PMID: 41022685 -
J Clin Invest
Mechanosensitive membrane domains regulate calcium entry in arterial endothelial cells to protect against inflammation. [Abstract]2024 May 21:e175057. PMID: 38771648 -
Biomater Res
Near-Infrared Light-Controlled Dynamic Hydrogel for Modulating Mechanosensitive Ion Channels in 3-Dimensional Environment. [Abstract]2025 Apr 9:29:0182. PMID: 40207256 -
Biofabrication
A mechanically active nucleus pulposus-on-a-chip for studying mechanobiology and therapeutic strategies in intervertebral disc disease. [Abstract]2026 Feb 5;18(1). PMID: 41587538 -
Cell Rep
Mechanosensitive calcium channels and integrins coordinate the reprogramming of colorectal cancer cells into a fetal-like state. [Abstract]2025 Sep 22;44(10):116308. PMID: 40986425 -
ACS Appl Bio Mater
Hyaluronic Acid Hydrogel with Adjustable Stiffness for Mesenchymal Stem Cell 3D Culture via Related Molecular Mechanisms to Maintain Stemness and Induce Cartilage Differentiation. [Abstract]2021 Mar 15;4(3):2601-2613. PMID: 35014377 -
Exp Cell Res
Investigating the effects of TRPV4 and Cav1.2 channels in 3D culture for promoting the differentiation of BMSCs at various stages. [Abstract]2025 Apr 1;447(1):114515. PMID: 40073957 -
Front Physiol
Transient Receptor Potential Cation Channel Subfamily V Member 4 Mediates Pyroptosis in Chronic Obstructive Pulmonary Disease. [Abstract]2021 Dec 24;12:783891. PMID: 35002766
GSK205 purchased from MedChemExpress. Usage Cited in: Front Physiol. 2021 Dec 24;12:783891. [Abstract]
LDH release induced by CSE was abrogated by pharmacological inhibition of TRPV4 with GSK 205 (10 μM).
GSK205 purchased from MedChemExpress. Usage Cited in: Front Physiol. 2021 Dec 24;12:783891. [Abstract]
Pharmacological inhibition with GSK 205 (10 μM) decreased the level of NLRP3, Pro-Caspase-1, Cleavage cspase-1, GSDMD, GSDMD-N induced by CSE.
GSK205 purchased from MedChemExpress. Usage Cited in: Front Physiol. 2021 Dec 24;12:783891. [Abstract]
Pharmacological inhibition with GSK 205 (10 μM) abrogated PI positive cell induced by CSE.
GSK205 purchased from MedChemExpress. Usage Cited in: Front Physiol. 2021 Dec 24;12:783891. [Abstract]
Increased IL-8, IL-1β, IL-18 mRNA expression induced by CSE were abrogated by pharmacological inhibition with GSK205 (10 μM).
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bioRxiv
Polarized Mechanosensitive Signaling Domains Protect Arterial Endothelial Cells Against Inflammation. [Abstract]2023 May 26:2023.05.26.542500. PMID: 37292837
溶剤 & 溶解度
DMSO : 250 mg/mL (519.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.32 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.32 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Ye L, et al. TRPV4 is a regulator of adipose oxidative metabolism, inflammation, and energy homeostasis. Cell. 2012 Sep 28;151(1):96-110. [Content Brief]
[2]. Kanju P, et al. Small molecule dual-inhibitors of TRPV4 and TRPA1 for attenuation of inflammation and pain. Sci Rep. 2016 Jun 1;6:26894. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0771 mL | 10.3853 mL | 20.7706 mL | 51.9265 mL |
| 5 mM | 0.4154 mL | 2.0771 mL | 4.1541 mL | 10.3853 mL | |
| 10 mM | 0.2077 mL | 1.0385 mL | 2.0771 mL | 5.1926 mL | |
| 15 mM | 0.1385 mL | 0.6924 mL | 1.3847 mL | 3.4618 mL | |
| 20 mM | 0.1039 mL | 0.5193 mL | 1.0385 mL | 2.5963 mL | |
| 25 mM | 0.0831 mL | 0.4154 mL | 0.8308 mL | 2.0771 mL | |
| 30 mM | 0.0692 mL | 0.3462 mL | 0.6924 mL | 1.7309 mL | |
| 40 mM | 0.0519 mL | 0.2596 mL | 0.5193 mL | 1.2982 mL | |
| 50 mM | 0.0415 mL | 0.2077 mL | 0.4154 mL | 1.0385 mL | |
| 60 mM | 0.0346 mL | 0.1731 mL | 0.3462 mL | 0.8654 mL | |
| 80 mM | 0.0260 mL | 0.1298 mL | 0.2596 mL | 0.6491 mL | |
| 100 mM | 0.0208 mL | 0.1039 mL | 0.2077 mL | 0.5193 mL |
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