FR167344 free base
目录号 : GC31926
FR167344freebase是有口服活性，非多肽的缓激肽受体B2(bradykininreceptorB2)拮抗剂，对B2有高亲和力，IC50值为65nM，对B1受体没有结合力。
Cas No.:215258-13-2
Sample solution is provided at 25 µL, 10mM.
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FR167344 free base is an orally active, nonpeptide bradykinin receptor B2 antagonist. FR167344 free base shows a high affinity binding to the B2 receptor with an IC50 value of 65 nM and no binding affinity for the B1 receptor.
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[1].
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[2].
[1]. Aramori I, et al. Novel subtype-selective nonpeptide bradykinin receptor antagonists FR167344 and FR173657. Mol Pharmacol. 1997 Feb;51(2):171-6. [2]. Asano M, et al. Effects of a nonpeptide bradykinin B2 receptor antagonist, FR167344, on different in vivoanimal models of inflammation.Br J Pharmacol. 1997 Dec;122(7):1436-40.
Kinase experiment: | Binding assays for the B1 and B2 receptor are carried out by using [3H]des-Arg10-kallidin and [3H]bradykinin, respectively. Cell membranes (12.5-75 mg/mLl) are incubated with various concentrations (saturation experiments) or 500 pM (displacement experiments) of [3H]des-Arg10-kallidin or [3H]bradykinin for 90 min in 0.25 mLof the binding solution containing 20 mM HEPES, pH 7.4, 125 mM N-methyl-D-glucamine, 5 mM KCl, 0.1% BSA, 1 mM 1,10-phenanthrolin monohydrate, 1 mM dithiothreitol, 1 mM captopril and 140 mg/mLbacitracin (for the B1 receptor) or 25 mM trimethylaminoethanesulfonic acid, pH 6.8, 0.1% BSA, 1 mM 1,10-phenanthrolin monohydrate, 1 mM dithiothreitol, 1 mM captopril, and 140 mg/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 1 mM 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[1]. |
Animal experiment: | Rat: Male Sprague-Dawley rats (8 weeks old) are deprived of food overnight and treated orally with FR167344, 15 min before carrageenin is injected into the right hind paw intraplantar. Paw volume is measuredby water plethysmometer before and 1, 2, 3 and 4 h afterthe injection of carrageenin. FR167344 is dissolved in 0.05N HCl and administered orally at a volume of 5 mL/kg. Carrageenin is made up as 1% solution in saline. Each rat received 0.1 mL of the irritant. As saline-control, saline is administered in the same manner as carrageenin.Mouse: Male ICR mice (Slc:ICR, 5 weeks old) are fasted overnight and used. Writhing responses are induced by an intraperitoneal injection of kaolin(250 mg/kg, 50 mL/kg). The responses are counted over a 10 or 15 min period by a trained observer. FR167344 dissolved in 0.05N HCl or vehicle (10 mL/kg) is administered orally 30 min before the intraperitoneal injection of kaolin. As saline-control, saline is administered in the same manner as kaolin[2]. |
References: [1]. Aramori I, et al. Novel subtype-selective nonpeptide bradykinin receptor antagonists FR167344 and FR173657. Mol Pharmacol. 1997 Feb;51(2):171-6. | |
| Cas No. | 215258-13-2 | SDF | |
| Canonical SMILES | O=C(N(C)C)C1=CC=C(/C=C/C(NCC(N(C2=CC=C(Cl)C(COC3=CC=CN4C3=NC(C)=C4Br)=C2Cl)C)=O)=O)C=C1 | ||
| 分子式 | C30H28BrCl2N5O4 | 分子量 | 673.38 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.485 mL | 7.4252 mL | 14.8505 mL |
| 5 mM | 0.297 mL | 1.485 mL | 2.9701 mL |
| 10 mM | 0.1485 mL | 0.7425 mL | 1.485 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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1. 首先保证母液是澄清的；
2.
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- Purity: >98.00%
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