GSK2798745
Based on 8 publication(s) in Google Scholar
GSK2798745 is a potent, selective, and orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker with IC50s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively. GSK2798745 can be used in cardiac and respiratory diseases research.
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- Purity: 99.80%
- CAS No.: 1419609-94-1
- 화학식: C25H28N6O3
- 분자량:460.53
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) GSK2798745
More- Nat Commun. 2023 Jun 23;14(1):3732. [Abstract]
- Adv Sci (Weinh). 2024 Apr 24:e2401583. [Abstract]
- JCI Insight. 2026 Jan 23;11(2):e182439. [Abstract]
- Acta Neuropathol Commun. 2025 Sep 29;13(1):205. [Abstract]
- J Physiol. 2026 Feb 28. [Abstract]
- Ann Thorac Surg. 2022 Apr;113(4):1256-1264. [Abstract]
- Exp Eye Res. 2023 Mar:228:109405. [Abstract]
- bioRxiv. 2023 Mar 16:2023.03.15.532784. [Abstract]
Biological Activity
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hTRPV4 1.8 nM (IC50) |
rTRPV4 1.6 nM (IC50) |
GSK2798745 inhibits TRPV4 agonist-induced impedance reduction in human umbilical vein endothelial cells (HUVECs)[3].
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.
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Animal Model:TRPV4-mediated lung edema in male Sprague-Dawley rats[3]
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Dosage:0, 16, 50, or 150 ng/kg
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Administration:Intravenous injection; 0, 16, 50, or 150 ng/kg per minute; 60 min
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Result:Inhibited the formation of pulmonary edema, with complete inhibition seen at the highest dose tested where the basal lung wet weight to body weight ratio was held to control levels (LW/BW=4.21).
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1419609-94-1
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Appearance Solid
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분자량 460.53
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화학식 C25H28N6O3
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Color Off-white to light yellow
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SMILES
N#CC1=CC=C2N=CN(C[C@](CCC3)(C)C[C@@]43CN(C5=NC=C(C(C)(O)C)N=C5)C(O4)=O)C2=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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Nat Commun
2023 Jun 23;14(1):3732. PMID: 37353484 -
Adv Sci (Weinh)
2024 Apr 24:e2401583. PMID: 38659239 -
JCI Insight
2026 Jan 23;11(2):e182439. PMID: 41574606 -
Acta Neuropathol Commun
2025 Sep 29;13(1):205. PMID: 41024271 -
J Physiol
In the gravid human uterus, oxytocin induces smooth muscle cell contraction via transient receptor potential vanilloid 4 channel activation. [Abstract]2026 Feb 28. PMID: 41762213 -
Ann Thorac Surg
Endothelial Transient Receptor Potential Vanilloid 4 Channels Mediate Lung Ischemia-Reperfusion Injury. [Abstract]2022 Apr;113(4):1256-1264. PMID: 33961815 -
Exp Eye Res
2023 Mar:228:109405. PMID: 36773739 -
bioRxiv
2023 Mar 16:2023.03.15.532784. PMID: 36993766
용액&용해도
DMSO : ≥ 100 mg/mL (217.14 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.43 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
순도&문서
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Data Sheet (281 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Goyal N, et al. Clinical Pharmacokinetics, Safety, and Tolerability of a Novel, First-in-Class TRPV4 Ion Channel Inhibitor, GSK2798745, in Healthy and Heart Failure Subjects. Am J Cardiovasc Drugs. 2019 Jun;19(3):335-342. [Content Brief]
[2]. Brooks CA, et al. Discovery of GSK2798745: A Clinical Candidate for Inhibition of Transient Receptor Potential Vanilloid 4 (TRPV4). ACS Med Chem Lett. 2019 Jul 15;10(8):1228-1233. [Content Brief]
[3]. Xiaoping Xu, et al. Identification of a Human Whole Blood-Based Endothelial Cell Impedance Assay for Assessing Clinical Transient Receptor Potential Vanilloid 4 Target Engagement Ex Vivo. J Pharmacol Exp Ther. 2021 Mar;376(3):436-443. [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 |
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| DMSO | 1 mM | 2.1714 mL | 10.8571 mL | 21.7141 mL | 54.2853 mL |
| 5 mM | 0.4343 mL | 2.1714 mL | 4.3428 mL | 10.8571 mL | |
| 10 mM | 0.2171 mL | 1.0857 mL | 2.1714 mL | 5.4285 mL | |
| 15 mM | 0.1448 mL | 0.7238 mL | 1.4476 mL | 3.6190 mL | |
| 20 mM | 0.1086 mL | 0.5429 mL | 1.0857 mL | 2.7143 mL | |
| 25 mM | 0.0869 mL | 0.4343 mL | 0.8686 mL | 2.1714 mL | |
| 30 mM | 0.0724 mL | 0.3619 mL | 0.7238 mL | 1.8095 mL | |
| 40 mM | 0.0543 mL | 0.2714 mL | 0.5429 mL | 1.3571 mL | |
| 50 mM | 0.0434 mL | 0.2171 mL | 0.4343 mL | 1.0857 mL | |
| 60 mM | 0.0362 mL | 0.1810 mL | 0.3619 mL | 0.9048 mL | |
| 80 mM | 0.0271 mL | 0.1357 mL | 0.2714 mL | 0.6786 mL | |
| 100 mM | 0.0217 mL | 0.1086 mL | 0.2171 mL | 0.5429 mL |
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