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

GSK2798745 

Cat. No.: HY-19765 Purity: 99.71%
COA Handling Instructions

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
Solution
10 mM * 1 mL in DMSO USD 765 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 765 In-stock
Solid
5 mg USD 695 In-stock
10 mg USD 1250 In-stock
50 mg USD 3750 In-stock
100 mg   Get quote  
200 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

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Based on 4 publication(s) in Google Scholar

GSK2798745 Related Antibodies

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TRPC TRPM TRPV TRPA TRPML

  • Biological Activity

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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].

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].

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

Appearance

Solid

Formula

C25H28N6O3
CAS No.
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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (542.85 mM; Need ultrasonic)

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
10 mM 0.2171 mL 1.0857 mL 2.1714 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.52 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.52 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.52 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.71%

COA (257 KB) LCMS (92 KB)

Handling Instructions (2659 KB)
References
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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.

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  • Dilution Calculator

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The dilution calculator equation

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This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

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

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