All AbMole products are for research use only, cannot be used for human consumption.
In vitro, Grapiprant inhibits [(3)H]PGE(2) binding to both human and rat EP(4) receptors with K(i) of 13 +/- 4 and 20 +/- 1 nM, respectively. Grapiprant is highly selective for the human EP(4) receptor over other human prostanoid receptor subtypes. Grapiprant also inhibits PGE(2)-evoked elevation in intracellular cAMP at the human and rat EP(4) receptors with pA(2) of 8.3 +/- 0.03 and 8.2 +/- 0.2 nM, respectively.
In vivo, oral administration of Grapiprant significantly reduces thermal hyperalgesia induced by intraplantar injection of PGE(2) (ED(50) = 12.8 mg/kg).
| Molecular Weight | 491.61 |
| Formula | C26H29N5O3S |
| CAS Number | 415903-37-6 |
| Solubility (25°C) | DMSO 10 mM |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Prostaglandin Receptor Products |
|---|
| Prostaglandin D2
Prostaglandin D2 (PGD2) is one of the major PGs actively produced in the brain of various mammals. PGD2 plays a protective role by suppressing inflammation. |
| Tafluprost acid
Tafluprost acid (AFP-172) is a selective prostanoid FP receptor agonist. Tafluprost acid shows a high affinity for human prostanoid FP receptor with Ki and EC50 values of 0.4 nM and 0.53 nM, respectively. Tafluprost acid has 126 times weaker binding affinity for prostanoid EP3 receptor (IC50=67 nM) than for the prostanoid FP receptor. |
| TG8-260
TG8-260 is a second-generation EP2 antagonist developed to alleviate the pathology of central nervous system and peripheral diseases driven by inflammation. |
| Camonagrel
Camonagrel is a compound that has inhibitory effects on Prostaglandin E2. |
| BAY 73-1449
BAY 73-1449 is a selective antagonist of prostacyclin receptor (IP), with high potency (IC50 of less than 0.1 nM) in cAMP assays in Human HEL cells and rat DRG. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
