Bermoprofen
(Synonyms: AD-1590) 目录号 : GC64075Bermoprofen (AD-1590) 是一种具有口服活性地非甾体类抗炎药。Bermoprofen 具有有效的解热作用,且生物半衰期短。Bermoprofen 是 LPS 诱导的兔发烧的有效拮抗剂。
Cas No.:78499-27-1
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Bermoprofen (AD-1590) is an orally active non-steroidal anti-inflammatory agent. Bermoprofen has potent antipyretic activities with a short biological half-life. Bermoprofen is a potent antagonist of LPS-induced fever in rabbits[1][2].
Bermoprofen (AD-1590) shows ulcerogenic activity as a side-effect like other nonsteroidal anti-inflammatory agents[1].
Bermoprofen (AD-1590) (0.04-0.1 mg/kg; p.o.) shows a dose-related antipyretic activity in LPS-induced febrile rabbits[2].
[1]. Mori M, et al. Prolongation of antipyretic action and reduction of gastric ulcerogenicity in the rat by controlled-release granules of bermoprofen, a new nonsteroidal anti-inflammatory drug. J Pharm Sci. 1991 Sep;80(9):876-80.
[2]. Nakamura H, et al. AD-1590, a potent antagonist of lipopolysaccharide-induced fever in rabbits. J Pharm Pharmacol. 1984 Mar;36(3):182-6.
Cas No. | 78499-27-1 | SDF | Download SDF |
别名 | AD-1590 | ||
分子式 | C18H16O4 | 分子量 | 296.32 |
溶解度 | 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。 |
||
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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.3747 mL | 16.8737 mL | 33.7473 mL |
5 mM | 0.6749 mL | 3.3747 mL | 6.7495 mL |
10 mM | 0.3375 mL | 1.6874 mL | 3.3747 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 | ||||||||||
计算重置 |
计算结果:
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,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Prolongation of antipyretic action and reduction of gastric ulcerogenicity in the rat by controlled-release granules of Bermoprofen, a new nonsteroidal anti-inflammatory drug
J Pharm Sci 1991 Sep;80(9):876-80.PMID:1800712DOI:10.1002/jps.2600800915.
While Bermoprofen [(+-)-10,11-dihydro-alpha,8-dimethyl-11- oxodibenz[b,f]oxepin-2-acetic acid], a new nonsteroidal antiinflammatory drug (NSAID), has potent antipyretic and analgesic activities with a short biological half-life, it shows ulcerogenic activity as a side-effect like other nonsteroidal anti-inflammatory drugs. A Bermoprofen preparation was specially designed to prolong its duration of action and to reduce its side effect. Immediate-release granules (IRGs) were prepared by coating particles of Nonpareil 103 with Bermoprofen. The IRGs were also coated by spraying a film solution composed of ethylcellulose and hydroxypropylmethylcellulose (3:2), and, thereby, three kinds of retard-release granules (RRGs) were obtained with the coating amounts of 1.5, 2.5, and 4%. Peak plasma Bermoprofen levels were seen 0.5, 1, 2, and 3 h after single oral administrations of IRG, RRG(1.5%), RRG (2.5%), and RRG(4%), respectively, in rats. The potency order in ulcerogenic activity was RRG(1.5%) greater than IRG greater than RRG(2.5%) greater than RRG(4%) after a single oral dosage in rats. Then, IRG and RRG(4%) were mixed (in the ratio 3:7, which was calculated from their simulated plasma Bermoprofen profiles) in order to get fast onset and long duration of antipyretic action. These mixed granules [i.e., the sustained-release granules (SRGs)] exhibited a falt plasma Bermoprofen profile, and longer lasting antipyretic and lower ulcerogenic activities in rats in comparison with IRG or Bermoprofen. From these results, it is suggested that a Bermoprofen SRG preparation has more durable therapeutic activity and lower side-effects as a NSAID.