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グラピプラント

グラピプラント 化學(xué)構(gòu)造式
415903-37-6
CAS番號(hào).
415903-37-6
化學(xué)名:
グラピプラント
別名:
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;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-メチルフェニルスルホニル)尿素
英語(yǔ)名:
Grapiprant
英語(yǔ)別名:
N-((4-(2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenethyl)carbamoyl)-4-methylbenzenesulfonamide;RQ 7;MR 10A7;AAT 007;CS-1556;Grprant;Grapiron;Graprant;Koplante;CJ-023423
CBNumber:
CB03054518
化學(xué)式:
C26H29N5O3S
分子量:
491.61
MOL File:
415903-37-6.mol

グラピプラント 物理性質(zhì)

融點(diǎn) :
>151°C (dec.)
比重(密度) :
1.29±0.1 g/cm3(Predicted)
貯蔵溫度 :
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)
酸解離定數(shù)(Pka):
5.19±0.10(Predicted)
外見 :
個(gè)體
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

安全性情報(bào)

グラピプラント 価格

メーカー 製品番號(hào) 製品説明 CAS番號(hào) 包裝 価格 更新時(shí)間 購(gòu)入

グラピプラント 化學(xué)特性,用途語(yǔ),生産方法

効能

抗炎癥薬, 抗リウマチ薬, プロスタグランジン受容體拮抗薬

説明

Prostaglandin E2 (PGE2) activates four E prostanoid (EP) receptors, EP1-4. EP4 is a Gs 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 (Ki = 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.

生物學(xué)の機(jī)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 上流と下流の製品情報(bào)

原材料

準(zhǔn)備製品


グラピプラント 生産企業(yè)

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415903-37-6(グラピプラント)キーワード:


  • 415903-37-6
  • 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
  • Grapiprant, 10 mM in DMSO
  • Grapiron
  • Graprant
  • Koplante
  • 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
  • 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-メチルフェニルスルホニル)尿素
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