1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. GSK726701A

GSK726701A 

Cat. No.: HY-112152 Purity: 98.72%
Handling Instructions

GSK726701A is a novel prostaglandin E2 receptor 4 (EP4) partial agonist with a pEC50 of 7.4.

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

GSK726701A Chemical Structure

GSK726701A Chemical Structure

CAS No. : 945721-87-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 550 In-stock
Estimated Time of Arrival: December 31
5 mg USD 500 In-stock
Estimated Time of Arrival: December 31
10 mg USD 850 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

GSK726701A is a novel prostaglandin E2 receptor 4 (EP4) partial agonist with a pEC50 of 7.4.

IC50 & Target

pEC50: 7.4[1]

In Vitro

GSK726701A has high selectivity (>100-fold) against a set of other prostaglandin receptors (EP1-3 , DP1 , FP, IP, TP) and no significant activity against a wider panel of targets. It demonstrates EP4 agonist activity with similar potency and intrinsic activity (pEC50=8.2) in a human whole blood (HWB) assay on the inhibition of LPS-mediated TNFα induction[1].

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

In Vivo

GSK726701A has good pharmacokinetic file in rat, dog and monkey. GSK726701A has robust activity in a range of animal models of inflammatory and neuropathic pain GSK726701A demonstrates a time-dependant, full reversal of CCI-induced mechanical allodynia at 3mg/kg, equivalent to the clinical gold standard gabapentin (30mg/kg). GSK726701A has an ED50 of 0.2mg/kg in the FCA acute rat model of inflammatory pain[1].

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

Molecular Weight

423.43

Formula

C₂₄H₂₂FNO₅

CAS No.

945721-87-9

SMILES

O=C1N(C2=CC=C(CC(O)=O)C(F)=C2)CC3=C(OCC)C4=CC=CC=C4C(OCC)=C31

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 : 25 mg/mL (59.04 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3617 mL 11.8083 mL 23.6167 mL
5 mM 0.4723 mL 2.3617 mL 4.7233 mL
10 mM 0.2362 mL 1.1808 mL 2.3617 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (5.90 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Rats[1]

The effect of GSK726701A (0.03-1mg/kg p.o. b.i.d. x5 days) is investigated on the FCA acute rat model of inflammatory pain[1].

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

References
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Keywords:

GSK726701AProstaglandin ReceptorInhibitorinhibitorinhibit

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Product Name:
GSK726701A
Cat. No.:
HY-112152
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