|
ChemicalBook Optimization Suppliers |
|
| 化学名: | ラフチジン | | 英語化学名: | Lafutidine | | 别名: | n-(4-(4-piperidinylmethyl)pyridyl-2-oxy)butenyl-2-(furfurylsulfinyl)acetamide;2-((Furan-2-ylMethyl)sulfinyl)-N-(4-((4-(piperidin-1-ylMethyl)pyridin-2-yl)oxy)but-2-en-1-yl)acetaMide;(Z)-2-((Furan-2-ylMethyl)sulfinyl)-N-(4-((3-(piperidin-1-ylMethyl)pyridin-2-yl)oxy)but-2-en-1-yl)acetaMide;Adefovir Dipivioxil;(Z)-2-((Furan-2-ylmethyl)sulfinyl)-N-(4-((3-(piperidin-1-ylmethyl)pyridin-2-yl)oxy)but-2-en-1-yl);(Z)-2-((Furan-2-ylmethyl)sulfinyl)-N-(4-((3-(piperidin-1-ylmethyl)pyridin-2-yl)oxy)but-2-en-1-;LAFUTIDINE(SUBJECTTOPATENTFREE);118288-08-07 | | CAS番号: | 118288-08-7 | | 分子式: | C22H29N3O4S | | 分子量: | 431.55 | | EINECS: | 601-513-8 | | カテゴリ情報: | Other APIs;Active Pharmaceutical Ingredients;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds | | Mol File: | 118288-08-7.mol |  |
| 融点 | 92.7-94.9° | | 沸点 | 704.2±60.0 °C(Predicted) | | 比重(密度) | 1.252±0.06 g/cm3(Predicted) | | 貯蔵温度 | Sealed in dry,Store in freezer, under -20°C | | 水溶解度 | Insoluble in water | | 溶解性 | DMF:5.0(Max Conc. mg/mL);11.59(Max Conc. mM)
DMSO:48.67(Max Conc. mg/mL);112.77(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:10):0.09(Max Conc. mg/mL);0.21(Max Conc. mM)
Ethanol:9.0(Max Conc. mg/mL);20.86(Max Conc. mM) | | 外見 | powder to crystal | | 酸解離定数(Pka) | 13.13±0.46(Predicted) | | 色 | White to Orange to Green | | CAS データベース | 118288-08-7(CAS DataBase Reference) |
| Sフレーズ | 24/25 | | HSコード | 29349990 |
| | ラフチジン Usage And Synthesis |
| 外観 | 白色～わずかにうすい黄色, 結晶性粉末～粉末 | | 溶解性 | エタノール及びアセトンに溶け、水にほとんど溶けない。 | | 用途 | ヒスタミンH2 受容体拮抗作
用を介して胃酸分泌抑制作用を示します。 | | 効能 | 消化性潰瘍薬, H2受容体拮抗薬 | | 商品名 | プロテカジン (大鵬薬品工業); プロテカジン (大鵬薬品工業) | | 説明 | Lafutidine was launched in Japan for the treatment of gastritis, reflux oesophagitis and
peptic ulcers. It can be prepared in eight steps from 4-(2-tetrahydropyranyloxy)-2(Z)-butenl-
ol. Lafutidine is a potent and longer-acting H2 antagonist compared to other marketed
compounds of its class such as cimetidine and famotidine. In contrast to other
commercially available H2 antagonists, lafutidine also exerts a gastroprotective action
probably via capsaicin-sensitive afferent nerves. It was clinically effective in the treatment
of nonsteroidal antiinflammatory drug-induced ulcer in patients refractory to existing
antiulcer agents. | | 説明 | Lafutidine is a histamine H2 receptor antagonist with gastroprotective activity. It inhibits histamine-induced cAMP production in CHO cells expressing human histamine H2 receptors when used at a concentration of 10 nM. Intragastric administration of lafutidine (3, 10, and 30 mg/kg) reduces hemorrhagic esophageal lesion size and gastric acid secretion in a rat model of pyloric ligation-induced reflux esophagitis. It prevents 5-fluorouracil-induced intestinal mucositis, diarrhea, and body weight loss in wild-type, but not Trpv1-/- or sensory deafferented, mice when administered at doses ranging from 3 to 30 mg/kg. Lafutidine (10 mg/kg) also reduces indomethacin-induced antral ulcer size in wild-type, but not chemically-deafferented, rats. | | Originator | Fujirebio (Japan) | | 使用 | Lafutidine, a newly developed histamine H(2)-receptor antagonist, inhibits gastric acid secretion | | 使用 | (Z)-2-((Furan-2-ylmethyl)sulfinyl)-n-(4-((3-(piperidin-1-ylmethyl)pyridin-2-yl)oxy)but-2-en-1-yl)acetamide is a Histaminic H2 receptor antagonists in ulcer disease. Also, it is a model compound used to investigate the binding mechanism between antiulcer drugs and human serum albumin (HSA). | | 使用 | Second generation histamine H2-receptor antagonist. Antiulcerative | | 定義 | ChEBI: Lafutidine is an organic molecular entity. | | brand name | Stogar, Protecadin |
|