首页 GPCR/G Protein Histamine Receptor FRG8701
FRG8701
编号 T11324    
CAS 108498-50-6     分子式 C22H30N2O4S     分子量 418.55
靶点: Histamine H2-receptor;
FRG8701 is a new Histamine H2-receptor antagonist with an IC50 of ranging from 0.25 to 0.43 μM.
选择批次  
纯度 98.00%
规格 库存 单价 数量
100 mg 待询 待询
500 mg 待询 待询
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生物活性

产品描述

FRG8701 is a new Histamine H2-receptor antagonist with an IC50 of ranging from 0.25 to 0.43 μM.

靶点活性

Histamine H2-receptor,0.25 to 0.43 μM

体外活性

The inhibitory potency of FRG8701 is almost the same as that of famotidine and approximately 33 times greater than that of cimetidine.Positive chronotropic response to histamine at 10-5 M is dose dependently inhibited by FRG8701 (FRG-8701) famotidine or cimetidine; and the IC50 values of FRG8701, famotidine and cimetidine are 3.3, 3.0 and 108.6 (×10-7M), respectively.

体内活性

Other necrotizing agents-induced gastric lesions are also inhibited by treatment of FRG8701. The oral ED50 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 ED50 values of FRG8701 for each ulcer model range from 1.7 to 6.9 mg/kg.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).

化学信息

分子量

418.55

分子式

C22H30N2O4S

CAS

108498-50-6

溶解度

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 2.389 ml 11.946 ml 23.892 ml
5 mM 0.478 ml 2.389 ml 4.778 ml
10 mM 0.239 ml 1.195 ml 2.389 ml
50 mM 0.048 ml 0.239 ml 0.478 ml
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