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

GSK2798745 

Cat. No.: HY-19765 Purity: 98.27%
Handling Instructions

GSK2798745 is a first-in-class, highly potent, selective, 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 is used in research for the treatment of pulmonary edema associated with congestive heart failure.

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
10 mM * 1 mL in DMSO USD 704 In-stock
Estimated Time of Arrival: December 31
5 mg USD 695 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1250 In-stock
Estimated Time of Arrival: December 31
50 mg USD 3750 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

GSK2798745 is a first-in-class, highly potent, selective, 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 is used in research for the treatment of pulmonary edema associated with congestive heart failure[1][2].

IC50 & Target

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

Clinical Trial
Molecular Weight

460.53

Formula

C₂₅H₂₈N₆O₃

CAS No.

1419609-94-1

SMILES

N#CC1=CC=C2N=CN(C[[email protected]](CCC3)(C)C[[email protected]@]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 provided by MCE.
References
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Keywords:

GSK2798745GSK 2798745GSK-2798745TRP ChannelTransient receptor potential channelsInhibitorinhibitorinhibit

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Product Name:
GSK2798745
Cat. No.:
HY-19765
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