| 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)
基本信息
|
产品编号：F10346 |
|||||
|
产品名称：FR167344 free base |
|||||
|
CAS: |
215258-13-2 |
储存条件 |
粉末 |
-20℃ |
四年 |
|
分子式： |
溶于液体 |
-80℃ |
六个月 |
||
|
分子量： |
673.38 |
|
|
||
|
化学名： |
|
||||
|
Solubility (25°C) |
体外 |
DMSO |
|
||
|
Ethanol |
|
||||
|
Water |
|
||||
|
体内（现配现用） |
|
|
|||
|
＜1mg/ml表示微溶或不溶。 |
|||||
|
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
|||||
|
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
|||||
生物活性
|
产品描述 |
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 |
65nM (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 65nM, 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 AFR167344 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 2.7mg/kg at 2h after carrageenin injection. Oral administration of FR167344 inhibits kaolin-induced writhing in mice with an ID50 of 2.8mg/kg in 10 min writhing and 4.2mg/kg in 15 min writhing. Oral administration of FR167344 inhibits caerulein-induced pancreatic oedema with an ID50 of 13.8mg/kg as well as increases in amylase and lipase of blood samples with ID50 of 10.3 and 7.4mg/kg,respectively, in rats. |
推荐实验方法(仅供参考)
|
激酶实验： |
|
Binding assays for the B1 and B2 receptor are carried out by using [3H]des-Arg10-kallidin and [3H]bradykinin, respectively.Cell membranes (12.5-75mg/mLl) are incubated with various concentrations (saturation experiments) or 500pM (displacement experiments) of [3H]des-Arg10-kallidin or [3H]bradykinin for 90 min in 0.25mLof the binding solution containing 20mM HEPES,pH 7.4, 125mM N-methyl-D-glucamine, 5mM KCl, 0.1% BSA, 1mM 1,10-phenanthrolin monohydrate, 1mM dithiothreitol, 1mM captopril and 140mg/mLbacitracin (for the B1 receptor) or 25mM trimethylaminoethanesulfonic acid, pH 6.8, 0.1% BSA, 1mM 1,10-phenanthrolin monohydrate, 1mM dithiothreitol, 1mM captopril, and 140mg/mLbacitracin (for the B2 receptor). All experiments are carried out at least three times in duplicate.The specific binding is calculated by subtracting the nonspecific binding, determined in the presence of 1mM unlabeled des-Arg10-kallidin (for the B1 receptor) or bradykinin (for the B2 receptor), from the total binding. The specific binding activity amounted to 90–92% of the total binding activity. |
|
动物实验: |
|
|
Mouse: Male ICR mice (Slc:ICR, 5 weeks old) are fasted overnight and used. Writhing responses are induced by an intraperitoneal injection of kaolin(250mg/kg, 50mL/kg). The responses are counted over a 10 or 15 min period by a trained observer. FR167344 dissolved in 0.05N HCl or vehicle (10mL/kg) is administered orally 30 min before the intraperitoneal injection of kaolin. As saline-control, saline is administered in the same manner as kaolin. |
|
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
