GSK2193874
Based on 19 publication(s) in Google Scholar
GSK2193874 is an orally active, potent, and selective TRPV4 antagonist with IC50s of 2 nM and 40 nM for rTRPV4 and hTRPV4.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.91%
- No. CAS: 1336960-13-4
- Fòrmula: C37H38BrF3N4O
- Peso molecular:691.62
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
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- Referencias
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Publications Citing Use of MedChemExpress (MCE) GSK2193874
More- Autophagy. 2021 Nov;17(11):3592-3606. [Abstract]
- J Nanobiotechnology. 2022 Jul 6;20(1):314. [Abstract]
- Acta Pharmacol Sin. 2023 Apr;44(4):811-821. [Abstract]
- Br J Pharmacol. 2025 Nov 2. [Abstract]
- J Ethnopharmacol. 2022 May 23:290:115105. [Abstract]
- Int J Pharm. 2026 Apr 10:694:126753. [Abstract]
- Int Immunopharmacol. 2026 Jun 10:185:116976. [Abstract]
- J Thorac Cardiovasc Surg. 2024 Oct;168(4):e121-e132. [Abstract]
- Cell Calcium. 2022 Jun;104:102590. [Abstract]
- J Leukoc Biol. 2023 Sep 1;114(3):266-279. [Abstract]
- Mol Immunol. 2023 May:157:176-185. [Abstract]
- Ultrasound Med Biol. 2025 Mar;51(3):494-507. [Abstract]
- J Cardiovasc Transl Res. 2023 Apr;16(2):414-426. [Abstract]
- Cryobiology. 2023 Dec:113:104569. [Abstract]
- Biol Bull. 2022 Feb;242(1):48-61. [Abstract]
- bioRxiv. 2026 Feb 20.
- Neuropharmacology and Therapy. 2025 Aug 23.
- SSRN. 2024 Jan 22.
- Research Square Print. 2022 Aug.
Customer Validation & Images
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Histological Imaging/Staining
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ELISA
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Cell Proliferation/Viability Assay
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WB
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Cell Imaging/Staining
Actividad biológica
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hTRPV4 2 nM (IC50) |
rTRPV4 40 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
0.04 μM
Compound: 28; GSK2193874
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Antagonist activity at human TRPV4 expressed in HEK293 cells assessed as inhibition of GSK634775A-induced calcium influx preincubated for 10 mins followed by GSK634775A addition by Fura-4 dye based FLIPR assay
Antagonist activity at human TRPV4 expressed in HEK293 cells assessed as inhibition of GSK634775A-induced calcium influx preincubated for 10 mins followed by GSK634775A addition by Fura-4 dye based FLIPR assay
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[PMID: 28523109] |
GSK2193874 is profiled against TRP channels and is selective against TRPV1, TRPA1, TRPC3, TRPC6, and TRPM8 (IC50>25 μM)[1]. GSK2193874 is a selective, orally active TRPV4 blocker that inhibits Ca2+ influx through recombinant TRPV4 channels and native endothelial TRPV4 currents. In whole-cell patch-clamp studies, GSK2193874 inhibits activation of recombinant TRPV4 currents when applied to the extracellular solution at 3 nM and above but is ineffective at up to 10 μM when applied to the inside of the cell by inclusion in the intracellular pipette solution[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1336960-13-4
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Appearance Solid
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Peso molecular 691.62
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Fòrmula C37H38BrF3N4O
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Color White to light yellow
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SMILES
O=C(C1=C(CN2CCC(N3CCCCC3)CC2)C(C4=CC=CC(C(F)(F)F)=C4)=NC5=CC(Br)=CC=C15)NC6(C7=CC=CC=C7)CC6
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (19)
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Journal Impact Factor
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Most Recent
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Autophagy
Cannabidiol inhibits human glioma by induction of lethal mitophagy through activating TRPV4. [Abstract]2021 Nov;17(11):3592-3606. PMID: 33629929
GSK2193874 purchased from MedChemExpress. Usage Cited in: Autophagy. 2021 Nov;17(11):3592-3606. [Abstract]
Effect of various ion channel inhibitors on CBD-induced glioma cell death. U251 or LN18 cells were pretreated with GSK2193874 (5 μM) for 1 h and then treated with CBD (30 μM) for 48 h. Cell viability was determined by the MTT assay.
GSK2193874 purchased from MedChemExpress. Usage Cited in: Autophagy. 2021 Nov;17(11):3592-3606. [Abstract]
Effect of TRPV4 inhibitor on CBD-induced mitophagy in glioma cells. U251 or U87 MG cells were treated with 20 μM CBD with or without GSK2193874 pretreatment (5 μM for 1 h), LC3 and Cl-PARP levels were analyzed by western blotting.
GSK2193874 purchased from MedChemExpress. Usage Cited in: Autophagy. 2021 Nov;17(11):3592-3606. [Abstract]
Effect of the TRPV4 inhibitor GSK2193874 (5 μM) on CBD-induced calcium flux in glioma cells. U251 or U87 MG cells were treated with 30 μM CBD with or without GSK2193874; Ca2+ flux was detected by using the Ca2+ indicator Fluro-4AM.
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J Nanobiotechnology
Protein nanoparticle-induced osmotic pressure gradients modify pulmonary edema through hyperpermeability in acute respiratory distress syndrome. [Abstract]2022 Jul 6;20(1):314. PMID: 35794575 -
Acta Pharmacol Sin
TRPV4 channel is involved in HSV-2 infection in human vaginal epithelial cells through triggering Ca2+ oscillation. [Abstract]2023 Apr;44(4):811-821. PMID: 36151392 -
Br J Pharmacol
ATP release and metabolism by human and guinea pig airways and P2X receptor-dependent effects on bronchopulmonary vagal afferent nerve subtypes. [Abstract]2025 Nov 2. PMID: 41178173 -
J Ethnopharmacol
Magnolol and honokiol target TRPC4 to regulate extracellular calcium influx and relax intestinal smooth muscle. [Abstract]2022 May 23:290:115105. PMID: 35157953 -
Int J Pharm
High viscosity microenvironment induces chemoresistance of cancer cells through upregulating P-gp. [Abstract]2026 Apr 10:694:126753. PMID: 41796944 -
Int Immunopharmacol
Transient receptor potential vanilloid 4 exacerbates sepsis-induced acute lung injury by promoting endothelial pyroptosis via the Ca2+/Nrf2/GSDMD signaling pathway. [Abstract]2026 Jun 10:185:116976. PMID: 42269552 -
J Thorac Cardiovasc Surg
Transient receptor potential vanilloid 4 channel inhibition attenuates lung ischemia-reperfusion injury in a porcine lung transplant model. [Abstract]2024 Oct;168(4):e121-e132. PMID: 38678474
GSK2193874 purchased from MedChemExpress. Usage Cited in: J Thorac Cardiovasc Surg. 2024 Oct;168(4):e121-e132. [Abstract]
Representative H&E-stained lung sections after 4 hours of reperfusion in vehicle- and GSK2193874 (GSK219) (30 mg/kg, p.o.)-treated recipient animals.
GSK2193874 purchased from MedChemExpress. Usage Cited in: J Thorac Cardiovasc Surg. 2024 Oct;168(4):e121-e132. [Abstract]
IL-8 levels in BAL fluid were significantly reduced in GSK2193874 (GSK219) (30 mg/kg,p.o.)-treated animals, however, IL-1β levels were not significantly altered.
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Cell Calcium
Blockage of transient receptor potential vanilloid 4 prevents postoperative atrial fibrillation by inhibiting NLRP3-inflammasome in sterile pericarditis mice. [Abstract]2022 Jun;104:102590. PMID: 35439615 -
J Leukoc Biol
Transient receptor potential vanilloid 4 (TRPV4) in neutrophils enhances myocardial ischemia/reperfusion injury. [Abstract]2023 Sep 1;114(3):266-279. PMID: 37232941 -
Mol Immunol
Low temperature reduces occludin expression in bronchial epithelial cells: Implications in cold-induced asthma. [Abstract]2023 May:157:176-185. PMID: 37044043 -
Ultrasound Med Biol
2025 Mar;51(3):494-507. PMID: 39632209 -
J Cardiovasc Transl Res
Roles of TRPV4 in Regulating Circulating Angiogenic Cells to Promote Coronary Microvascular Regeneration. [Abstract]2023 Apr;16(2):414-426. PMID: 36103035 -
Cryobiology
Effects of spray cryotherapy on cough receptors and airway microenvironment in a canine model of chronic bronchitis. [Abstract]2023 Dec:113:104569. PMID: 37597598 -
Biol Bull
Functional Characterization of TRPV-Like Ion Channels Involved in Nematocyst Discharge from the Sea Anemone Diadumene lineata. [Abstract]2022 Feb;242(1):48-61. PMID: 35245164 -
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Solvente y solubilidad
DMSO : 100 mg/mL (144.59 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. 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. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Protocolo
Rats[2]
Adult male Sprague-Dawley rats (n=7 to 8 per group) are treated with vehicle (6% Cavitron) or GSK2193874 (30 mg/kg per day) via oral gavage for at least 4 days before osmotic challenges. Rats undergo acute and chronic hyper- and hypo-osmotic challenges. Sprague-Dawley rats are administered vehicle (0.9% NaCl, 25 mL/kg), NSC 269420 (30 mg/kg), or hydrochlorothiazide (30 mg/kg) via oral gavage. Urine is then collected over 4 hours followed by blood sampling. Rats recover for 4 days and then receive GSK2193874 (30 mg/kg per day oral gavage) for 5 days before repeating the diuretic challenge.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Cheung M, et al. Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4. ACS Med Chem Lett. 2017 Mar 20;8(5):549-554. [Content Brief]
[2]. Thorneloe KS, et al. An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure. Sci Transl Med. 2012 Nov 7;4(159):159ra148. [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. 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 | 1.4459 mL | 7.2294 mL | 14.4588 mL | 36.1470 mL |
| 5 mM | 0.2892 mL | 1.4459 mL | 2.8918 mL | 7.2294 mL | |
| 10 mM | 0.1446 mL | 0.7229 mL | 1.4459 mL | 3.6147 mL | |
| 15 mM | 0.0964 mL | 0.4820 mL | 0.9639 mL | 2.4098 mL | |
| 20 mM | 0.0723 mL | 0.3615 mL | 0.7229 mL | 1.8074 mL | |
| 25 mM | 0.0578 mL | 0.2892 mL | 0.5784 mL | 1.4459 mL | |
| 30 mM | 0.0482 mL | 0.2410 mL | 0.4820 mL | 1.2049 mL | |
| 40 mM | 0.0361 mL | 0.1807 mL | 0.3615 mL | 0.9037 mL | |
| 50 mM | 0.0289 mL | 0.1446 mL | 0.2892 mL | 0.7229 mL | |
| 60 mM | 0.0241 mL | 0.1205 mL | 0.2410 mL | 0.6025 mL | |
| 80 mM | 0.0181 mL | 0.0904 mL | 0.1807 mL | 0.4518 mL | |
| 100 mM | 0.0145 mL | 0.0723 mL | 0.1446 mL | 0.3615 mL |
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