Grapiprant (CJ-023423) - CAS 415903-37-6
Catalog number: B0084-470919
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C26H29N5O3S
Molecular Weight:
491.61
COA:
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Targets:
Prostaglandin Receptor
Description:
Grapiprant, also known as CJ-023,423, RQ-00000007 and AAT-007, is a novel, potent and selective prostaglandin EP4 receptor antagonist with antihyperalgesic properties.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-470919 10 mg $198 In stock
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Purity:
98%
Appearance:
Solid powder
Synonyms:
CJ-023423; CJ 023423; CJ023423; CAS#415903-37-6; RQ-00000007; RQ 00000007; RQ00000007; AAT-007; AAT007; AAT 007; Grapiprant
Solubility:
Soluble in DMSO, not in water
Storage:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
MSDS:
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Shelf Life:
2 years if stored properly
Canonical SMILES:
O=C(NCCC1=CC=C(C=C1)N2C(CC)=NC3=C(N=C(C=C32)C)C)NS(C4=CC=C(C=C4)C)(=O)=O
1.Grapiprant: an EP4 prostaglandin receptor antagonist and novel therapy for pain and inflammation.
Kirkby Shaw K;Rausch-Derra LC;Rhodes L Vet Med Sci. 2015 Dec 21;2(1):3-9. doi: 10.1002/vms3.13. eCollection 2016 Feb.
There are five active prostanoid metabolites of arachidonic acid (AA) that have widespread and varied physiologic functions throughout the body, including regulation of gastrointestinal mucosal blood flow, renal haemodynamics and primary haemostasis. Each prostanoid has at least one distinct receptor that mediates its action. Prostaglandin E;2; (PGE ;2;) is a prostanoid that serves important homeostatic functions, yet is also responsible for regulating pain and inflammation. PGE ;2; binds to four receptors, of which one, the EP4 receptor, is primarily responsible for the pain and inflammation associated with osteoarthritis (OA). The deleterious and pathologic actions of PGE ;2; are inhibited in varying degrees by steroids, aspirin and cyclo-oxygenase inhibiting NSAIDs; however, administration of these drugs causes decreased production of PGE ;2;, thereby decreasing or eliminating the homeostatic functions of the molecule. By inhibiting just the EP4 receptor, the homeostatic function of PGE ;2; is better maintained. This manuscript will introduce a new class of pharmaceuticals known as the piprant class. Piprants are prostaglandin receptor antagonists (PRA). This article will include basic physiology of AA, prostanoids and piprants, will review available evidence for the relevance of EP4 PRAs in rodent models of pain and inflammation, and will reference available data for an EP4 PRA in dogs and cats.
2.Detection and quantification of the selective EP4 receptor antagonist CJ-023423 (grapiprant) in canine plasma by HPLC with spectrofluorimetric detection.
Vito V;Saba A;Lee HK;Owen H;Poapolathep A;Giorgi M J Pharm Biomed Anal. 2016 Jan 25;118:251-258. doi: 10.1016/j.jpba.2015.11.004. Epub 2015 Nov 7.
Grapiprant, a novel pharmacologically active ingredient, acts as a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2). It is currently under development for use in humans and dogs for the control of pain and inflammation associated with osteoarthritis. The aim of the present study was to develop an easy and sensitive method to quantify grapiprant in canine plasma and to apply the method in a canine patient. Several parameters, both in the extraction and detection method were evaluated. The final mobile phase consisted of ACN:AcONH4 (20 mM) solution, pH 4 (70:30, v/v) at a flow rate of 1 mL/min. The elution of grapiprant and IS (metoclopramide) was carried out in isocratic mode through a Synergi Polar-RP 80A analytical column (150 mm × 4.6 mm). The best excitation and emission wavelengths were 320 and 365 nm, respectively. Grapiprant was extracted from the plasma using CHCl3, which gave a recovery of 88.1 ± 10.22% and a lower limit of quantification (LLOQ) of 10 ng/mL. The method was validated in terms of linearity, limit of detection (LOD), LLOQ, selectivity, accuracy and precision, extraction recovery, stability, and inter-laboratory cross validation, according to international guidelines.
3.CJ-023,423, a novel, potent and selective prostaglandin EP4 receptor antagonist with antihyperalgesic properties.
Nakao K;Murase A;Ohshiro H;Okumura T;Taniguchi K;Murata Y;Masuda M;Kato T;Okumura Y;Takada J J Pharmacol Exp Ther. 2007 Aug;322(2):686-94. Epub 2007 May 10.
The prostaglandin (PG) EP(4) receptor subtype is expressed by peripheral sensory neurons. Although a potential role of EP(4) receptor in pain has been suggested, a limited number of selective ligands have made it difficult to explore the physiological functions of EP(4) or its potential as a new analgesic target. Here, we describe the in vitro and in vivo pharmacology of a novel EP(4) receptor antagonist, N-[({2-[4-(2-ethyl-4,6-dimethyl-1H-imidazo [4,5-c] pyridin-1-yl) phenyl]ethyl}amino) carbonyl]-4-methylbenzenesulfonamide (CJ-023,423). In vitro, CJ-023,423 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. CJ-023,423 is highly selective for the human EP(4) receptor over other human prostanoid receptor subtypes. It 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 CJ-023,423 significantly reduces thermal hyperalgesia induced by intraplantar injection of PGE(2) (ED(50) = 12.8 mg/kg). CJ-023,423 is also effective in models of acute and chronic inflammatory pain. CJ-023,423 significantly reduces mechanical hyperalgesia in the carrageenan model.
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CAS 415903-37-6 Grapiprant (CJ-023423)

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