2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. GSK2798745

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.

For research use only. We do not sell to patients.

GSK2798745 Chemical Structure

GSK2798745 Chemical Structure

CAS No. : 1419609-94-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 765 In-stock
Solution
10 mM * 1 mL in DMSO USD 765 In-stock
Solid
1 mg USD 278 In-stock
5 mg USD 695 In-stock
10 mg USD 1250 In-stock
50 mg USD 2980 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 5 publication(s) in Google Scholar

GSK2798745 Related Antibodies

Top Publications Citing Use of Products

View All TRP Channel Isoform Specific Products:

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TRPC TRPM TRPV TRPA TRPML

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3].

IC50 & Target

IC50: 1.8 nM (hTRPV4) and 1.6 nM (rTRPV4)[2]
In Vitro

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.

GSK2798745 Related Antibodies
In Vivo

GSK2798745 inhibits TRPV4 agonist-mediated lung edema in rats in a dose-dependent manner[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: TRPV4-mediated lung edema in male Sprague-Dawley rats[3]
Dosage: 0, 16, 50, or 150 ng/kg
Administration: Intravenous injection; 0, 16, 50, or 150 ng/kg per minute; 60 min
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).
Clinical Trial
Molecular Weight

460.53

Formula

C25H28N6O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1714 mL 10.8571 mL 21.7141 mL
5 mM 0.4343 mL 2.1714 mL 4.3428 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.80%

COA (257 KB) HNMR (269 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

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 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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GSK2798745 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK27987451419609-94-1GSK 2798745GSK-2798745TRP ChannelTransient receptor potential channelshuman umbilical vein endothelial cellsHUVECscardiacrespiratoryInhibitorinhibitorinhibit

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