BAY-u 9773
目录号 : GC10266Antagonist of CysLT1/CysLT2 receptors
Cas No.:154978-38-8
Sample solution is provided at 25 µL, 10mM.
BAY-u9773, an antagonist of cysteinyl leukotriene (Cys-LT) receptor, which have equal affinity towards CysLT1 and CysLT2 receptors.
The Cys-LTs are a family of potent bioactive lipids, acting through two distinct G protein-coupled receptors named the CysLT1 and CysLT2 receptors.
To determine the profile of BAY-u9773 as a Cys-LT receptor antagonist, the effect of this component on different smooth muscle preparations was investigated. The result showed that BAY u9773 antagonised 'typical' cysteinyl-leukotriene receptors and inhibited bronchial and venous muscle contractions in the human muscle preparations [1].
BAY-u9773 was also extensively used in animal model to study the function of CysLT1 and CysLT2 receptors. For instance, BAY-u9773 treatment inhibited the infiltration of eosinophil in BAL Fluid in a model of OVA-induced airway hypersensitivity and inflammation in guinea pigs [2]. In addition, this components was shown to act as competitive antagonist towards LTC4 and LTE4 receptors and results in contractions in trachea of guinea pig models [3].
References:
1. Tudhope SR, Cuthbert NJ, Abram TS, Jennings MA, Maxey RJ, Thompson AM, et al. BAY u9773, a novel antagonist of cysteinyl-leukotrienes with activity against two receptor subtypes. Eur J Pharmacol 1994,264:317-323.
2. Muraki M, Imbe S, Santo H, Sato R, Sano H, Iwanaga T, et al. Effects of a cysteinyl leukotriene dual 1/2 receptor antagonist on antigen-induced airway hypersensitivity and airway inflammation in a guinea pig asthma model. Int Arch Allergy Immunol 2011,155 Suppl 1:90-95.
3. Wikstrom Jonsson E, Rosenqvist U, Dahlen SE. Agonist and antagonist activities of the leukotriene analogue BAY u9773 in guinea pig lung parenchyma. Eur J Pharmacol 1998,357:203-211.
Cas No. | 154978-38-8 | SDF | |
化学名 | 4-(((4S,5R,6E,8E,10E,13E)-1-carboxy-4-hydroxynonadeca-6,8,10,13-tetraen-5-yl)thio)benzoic acid | ||
Canonical SMILES | O[C@H]([C@@H](/C=C/C=C/C=C/C/C=C/CCCCC)SC1=CC=C(C(O)=O)C=C1)CCCC(O)=O | ||
分子式 | C27H36O5S | 分子量 | 472.64 |
溶解度 | DMF: 25 mg/ml,DMSO: 25 mg/ml,Ethanol: 25 mg/ml,PBS (pH 7.2): .15 mg/ml | 储存条件 | Store at -80°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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.1158 mL | 10.5789 mL | 21.1578 mL |
5 mM | 0.4232 mL | 2.1158 mL | 4.2316 mL |
10 mM | 0.2116 mL | 1.0579 mL | 2.1158 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 | |||
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% 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。
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