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

GSK726701A 

Cat. No.: HY-112152
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

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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].

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].

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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
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

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GSK726701A
Cat. No.:
HY-112152
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GSK726701A

Cat. No.: HY-112152