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108498-50-6

中文名稱 108498-50-6
英文名稱 FRG 8701
CAS 108498-50-6
分子式 C22H30N2O4S
分子量 418.55
MOL 文件 108498-50-6.mol
108498-50-6 結構式 108498-50-6 結構式

基本信息

中文別名
化合物 T11324
英文別名
FRG 8701
Acetamide, 2-[(2-furanylmethyl)sulfinyl]-N-[3-[3-(1-piperidinylmethyl)phenoxy]propyl]-

物理化學性質

沸點675.2±55.0 °C(Predicted)
密度1.226±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
酸度系數(pKa)13.77±0.46(Predicted)

常見問題列表

生物活性
FRG-8701 是一種新組氨酸 H2-receptor 拮抗劑,IC50 值為 0.25 至 0.43 μM。
靶點

IC50: 0.25 to 0.43 μM (Histamine H 2 -receptor)

體外研究

Positive chronotropic response to histamine at 10 -5 M is dose dependently inhibited by FRG8701 (FRG-8701) famotidine or cimetidine; and the IC 50 values of FRG8701, famotidine and cimetidine are 3.3, 3.0 and 108.6 (×10 -7 M), respectively.The inhibitory potency of FRG8701 is almost the same as that of famotidine and approximately 33 times greater than that of cimetidine.

體內研究

In the pylorus-ligated (4 hr) rats, each drug, given intraduodenally, dose-dependently inhibits the total acid output. FRG8701 at 10 or 30 mg/kg, given orally or intraperitoneally, significantly prevent the formation of the gastric mucosal lesions induced by 0.4 N HCI+50% ethanol (HCI?ethanol). Other necrotizing agents-induced gastric lesions are also inhibited by treatment of FRG8701. The oral ED 50 values against the lesions range from 1.1 to 9.4 mg/kg. FRG8701, given orally, dose-dependently prevents the development of gastric lesions induced by stress and indomethacin. Duodenal ulcer induced by mepirizole is also inhibited with FRG8701. The ED 50 values of FRG8701 for each ulcer model range from 1.7 to 6.9 mg/kg.

"108498-50-6" 相關產品信息
118288-14-5 108498-50-6
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