945721-87-9
945721-87-9 structure
- Name: GSK726701A
- Chemical Name: GSK726701A
- CAS Number: 945721-87-9
- Molecular Formula: C24H22FNO5
- Molecular Weight: 423.43
- Catalog: Signaling Pathways GPCR/G Protein Prostaglandin Receptor
- Create Date: 2019-02-17 18:23:45
- Modify Date: 2024-01-10 16:50:46
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GSK726701A is a novel prostaglandin E2 receptor 4 (EP4) partial agonist with a pEC50 of 7.4.
| Name | GSK726701A |
|---|
| Description | GSK726701A is a novel prostaglandin E2 receptor 4 (EP4) partial agonist with a pEC50 of 7.4. |
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| Related Catalog | |
| 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]. |
| Animal Admin | 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]. |
| References |
| Molecular Formula | C24H22FNO5 |
|---|---|
| Molecular Weight | 423.43 |