グラピプラント化学構造式

グラピプラント

化学名:グラピプラント

CAS番号.415903-37-6

英語名:Grapiprant

CBNumberCB03054518

MFC26H29N5O3S

MW491.61

MOL File415903-37-6.mol

别名

グラピプラント

1-[2-(4-{2-エチル-4,6-ジメチル-1H-イミダゾ[4,5-c]ピリジン-1-イル}フェニル)エチル]-3-(4-メチルベンゼンスルホニル)尿素

1-[2-(4-{2-エチル-4,6-ジメチルイミダゾ[4,5-c]ピリジン-1-イル}フェニル)エチル]-3-(4-メチルベンゼンスルホニル)尿素

グラピプラント物理性質

融点	>151°C (dec.)
比重(密度)	1.29±0.1 g/cm3(Predicted)
貯蔵温度	Sealed in dry,Store in freezer, under -20°C
溶解性	DMSO に可溶 (少なくとも 10 mg/ml まで)
酸解離定数(Pka)	5.19±0.10(Predicted)
外見	個体
色	オフホワイト
安定性：	-20°C の DMSO 溶液で最大 3 か月間保存できます。
InChIKey	HZVLFTCYCLXTGV-UHFFFAOYSA-N
SMILES	C1(S(NC(NCCC2=CC=C(N3C4C=C(C)N=C(C)C=4N=C3CC)C=C2)=O)(=O)=O)=CC=C(C)C=C1

グラピプラント化学特性,用途語,生産方法

効能
抗炎症薬, 抗リウマチ薬, プロスタグランジン受容体拮抗薬
説明
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.
使用
CJ-023423 is a potent and selective antagonist of E prostanoid 4 (EP4) receptor.
生物学の機能
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).
副作用
Possible side effects of Grapiprant include: vomiting, drowsiness, diarrhoea, loss of appetite, blood or mucus in the stool, and reduced blood protein levels. The degree of reaction can vary from mild to severe, but if your dog experiences a loss of appetite or abnormal faeces, you should contact your veterinarian promptly.

グラピプラント生産企業

415903-37-6, グラピプラントキーワード

Send Inquriy

グラピプラント

グラピプラント 化学特性,用途語,生産方法

グラピプラント 生産企業

415903-37-6, グラピプラント キーワード

グラピプラント化学特性,用途語,生産方法

グラピプラント生産企業

415903-37-6, グラピプラントキーワード