Grapiprant

Grapiprant Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

Prostaglandin E₂ (PGE₂) activates four E prostanoid (EP) receptors, EP_1-4. EP₄ is a G_s protein-coupled receptor that, by elevating the second messenger cAMP, plays important roles in bone formation and resorption, cancer, and atherosclerosis. CJ-023423 is a potent and selective antagonist of the EP₄ receptor (K_i = 13 and 20 nM for human and rat EP₄, respectively). It inhibits PGE₂-evoked elevation in intracellular cAMP in cells and, in vivo, reduces thermal hyperalgesia induced by intraplantar injection of PGE₂. CJ-023423 reduces acute and chronic inflammatory pain in different mouse models.

Verwenden

CJ-023423 is a potent and selective antagonist of E prostanoid 4 (EP4) receptor.

Biologische Funktion

Grapiprant (CJ-023423) is an orally available, a potent and selective EP4 receptor antagonist that exhibits significant inhibitory effects on paw swelling, inflammatory biomarkers, synovial inflammation and bone destruction in AIA rats. Grapiprant is highly selective for the human EP4 receptor over other human prostanoid receptor subtypes. It also inhibits PGE2-evoked elevation in intracellular cAMP at the human and rat EP4 receptors with pA2 of 8.3 and 8.2 nM, respectively. In vivo, oral administration of grapiprant significantly reduces thermal hyperalgesia induced by intraplantar injection of PGE2 (ED50 = 12.8 mg/kg). It is also effective in models of acute and chronic inflammatory pain. Grapiprant significantly reduces mechanical hyperalgesia in the carrageenan model. Furthermore, it significantly reverses complete Freund′s adjuvant-induced chronic inflammatory pain response. It produces antihyperalgesic effects in animal models of inflammatory pain. Grapiprant is approved and widely used for treatment of osteoarthritis related pain in dogs. Grapiprant is classify as a non-cyclooxygenase inhibiting non-steroidal anti-inflammatory drug (NSAID).

Grapiprant Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

Grapiprant Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
Hpets Biotech Company (Chongqing) Co.,ltd	+8613340353813	info@hanpets.com	China	26	58
Hangzhou ICH Biofarm Co., Ltd	+86-0571-28186870; +undefined8613073685410	sales@ichemie.com	China	985	58
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32715	60
BOC Sciences	+1-631-485-4226	inquiry@bocsci.com	United States	19553	58
TopScience Biochemical	00852-68527855	info@itopbiochem.com	China Hong Kong	902	58
ANHUI WITOP BIOTECH CO., LTD	+8615255079626	eric@witopchemical.com	China	23556	58
Guangzhou TongYi biochemistry technology Co.,LTD	+8613073028829	mack@tongyon.com	China	2996	58
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn	United States	6393	58
Nanjing Doge Biomedical Technology Co., Ltd	+86-25-58227606 +86-15305155328	sales@dogechemical.com	China	4128	58
LEAP CHEM CO., LTD.	+86-852-30606658	market18@leapchem.com	China	24738	58

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• CJ-023423
• Grapiprant
• 2-Ethyl-4,6-dimethyl-1-[4-[2-[[[[(4-methylphenyl)sulfonyl]amino]carbonyl]amino]ethyl]phenyl]-1H-imidazo[4,5-c]pyridine
• AAT 007
• MR 10A7
• RQ 00000007
• RQ 7
• Grapiprant (CJ-023423)
• 1-[2-[4-(2-ethyl-4,6-dimethylimidazo[4,5-c]pyridin-1-yl)phenyl]ethyl]-3-(4-methylphenyl)sulfonylurea
• CAS#415903-37-6
• CJ-023423; CJ 023423; CJ023423; CAS#415903-37-6; RQ-00000007; RQ 00000007; RQ00000007; AAT-007; AAT007; AAT 007; GRAPIPRANT
• CS-1556
• GRAPIPRANT;RQ-00000007;AAT-007
• Grprant
• N-((4-(2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenethyl)carbamoyl)-4-methylbenzenesulfonamide
• N-[[2,4-(2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenylethylamino]carbonyl]-4-methyl-benzenesulfonamide
• RQ 00000007,Inhibitor,Grapiprant,CJ 023423,RQ00000007,Prostaglandin Receptor,AAT 007,inhibit,AAT007,CJ023423
• Grapiprant, CJ-023423, AAT-007
• 415903-37-6
• API