| 中文名称: | FR167344 free base | ||||
|---|---|---|---|---|---|
| 英文名称: | FR167344 free base | ||||
| CAS No: | 215258-13-2 | 分子式: | C30H28BrCl2N5O4 | 分子量: | 673.38 |
| CAS No: | 215258-13-2 | ||||
| 分子式: | C30H28BrCl2N5O4 | ||||
| 分子量: | 673.38 | ||||
![[Des-Arg9]-缓激肽](http://struc.chem960.com/strucimg/16000/le1hdxlxgxjlsxqt3o6cbqee.png)
包装规格：
5mg in glass bottle
产品简介：
一种有口服活性，非多肽的缓激肽受体B2 (bradykinin receptor B2) 拮抗剂，对B2有高亲和力，IC50值为65nM，对B1受体没有结合力。
靶点：
IC50: 65 nM (Bradykinin receptor B2)
体外研究：
In competitive experiments using membranes prepared from Chinese hamster ovary cells expressing the bradykinin receptor subtypes, FR167344 shows a high affinity binding to the B2 receptor with IC50 values of 65 nM, and no binding affinity for the B1 receptor. FR167344 inhibits the B2 receptor-mediated phosphatidylinositol (PI) hydrolysis and produces a concentration-dependent rightward shift in the dose-response curve to bradykinin. This shift is accompanied by a progressive reduction of maximal response. Estimated pA2 values for the antagonism of bradykinin induced PI hydrolysis by FR167344 is 8.0. FR167344 shows no stimulatory effects on PI hydrolysis.
体内研究：
Oral administration of FR167344 inhibits carrageenin-induced paw oedema in rats with an ID50 of 2.7 mg/kg at 2h after carrageenin injection. Oral administration of FR167344 inhibits kaolin-induced writhing in mice with an ID50 of 2.8 mg/kg in 10 min writhing and 4.2 mg/kg in 15 min writhing. Oral administration of FR167344 inhibits caerulein-induced pancreatic oedema with an ID50 of 13.8 mg/kg as well as increases in amylase and lipase of blood samples with ID50 of 10.3 and 7.4 mg/kg, respectively, in rats.
保存条件：
-20℃
注意事项：
1、为了您的安全和健康，请穿实验服并戴一次性手套操作。
2、以上信息仅做参考交流之用。
2、以上信息仅做参考交流之用。
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安全说明：
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