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Grapiprant CJ-023423 RQ-00000007 AAT-007 415903-37-6
Grapiprant is an EP4 receptor antagonist.
| Cas No. | 415903-37-6 |
| Synonyms | RQ-00000007 |
| Chemical Name | N-[[2,4-(2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenylethylamino]carbonyl]-4-methyl-benzenesulfonamide |
| Canonical SMILES | O=C(NS(C1=CC=C(C)C=C1)(=O)=O)NCCC2=CC=C(N3C(CC)=NC4=C(C)N=C(C)C=C43)C=C2 |
| Formula | C26H29N5O3S |
| M.Wt | 491.6 |
| Storage | Store at -20°C |
| Solubility | ≤10mg/ml in ethanol;10mg/ml in DMSO;20mg/ml in dimethyl formamide |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month. |
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. | |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prostaglandin E2 (PGE2) can activate 4 E prostanoid (EP) receptors, namded EP1-4. EP4, a Gs protein-coupled receptor, plays key roles in cancer, bone formation and resorption, as well as atherosclerosis by elevating the second messenger cAMP.
In vitro: In vitro, CJ-023,423 was able to inhibit [(3)H]PGE(2) binding to both human and rat EP(4) receptors. CJ-023,423 was found to be highly selective for the human EP(4) receptor over other human prostanoid receptor subtypes. CJ-023,423 also inhibited PGE(2)-evoked elevation in intracellular cAMP at the human and rat EP(4) receptors with pA(2) of 8.3 and 8.2 nM, respectively [1].
In vivo: In vivo, po administration of CJ-023,423 could significantly reduce the thermal hyperalgesia that was induced by i.p. injection of PGE(2). CJ-023,423 was also effective in models of acute and chronic inflammatory pain. In addition, CJ-023,423 was able to significantly reduce mechanical hyperalgesia in the carrageenan model. Furthermore, CJ-023,423 reversed complete Freund's adjuvant-induced chronic inflammatory pain response significantly [1].
Clinical trial: A study of the effect of CJ-023,423 on the incidence of stomach ulcers has been completed but no result is release. Another phase II trial of CJ-023,423 in advanced solid tumors is proposed [https://clinicaltrials.gov/ct2/results term=CJ-023423&Search=Search].
Reference:
[1] Nakao, K. ,Murase, A.,Ohshiro, H., et al. CJ-023,423, a novel, potent and selective prostaglandin EP4 receptor antagonist with antihyperalgesic properties. Journal of Pharmacology and Experimental Therapeutics 322(2), 686-694 (2007).
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.