REV 5901
目录号 : GC14939
An antagonist of cysteinyl-leukotriene receptors
Cas No.:101910-24-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Ki: 0.7 μM for cysteinyl-leukotriene receptor of guinea pig lung membranes
REV 5901 is an antagonist of cysteinyl-leukotriene receptors.
Cysteinyl leukotriene receptor 1, a receptor for cysteinyl leukotrienes, contributes to mediating various allergic and hypersensitivity reactions by binding the cysteinyl LTs (CysLTs; viz, LTC4, LTD4, and to a much lesser extent, LTE4) in humans and models of the reactions in other animals.
In vitro: Previous in-vitro showed that REV 5901 had a Ki value of 0.7 μM vs. [3H]leukotriene D4 ([3H]-LTD4) binding to membranes from guinea pig lung. Against LTC4-, LTD4- and LTE4-induced contractions of guinea pig parenchymal strips, REV 5901 had Kb values of ca 3 μM and was relatively ineffective against contractions that was induced by other spasmogens. Moreover, in isolated guinea pig hearts, the peptiodoleukotriene-antagonist activity was also observed against the hemodynamic and vasoconstriction effects of LTD4. In addition, unlike other reported antagonists, REV 5901 was found to be ineffective against the multiple forms of cyclic nucleotide phosphodiesterases [1].
In vivo: Animal study found that the oral antagonist activity had been shown with an LTD4-induced bronchoconstriction model and with an LTD4-induced wheal response model in guinea pigs [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Van Inwegen, R. G.,Khandwala, A.,Gordon, R., et al. REV 5901: An orally effective peptidoleukotriene antagonist, detailed biochemical/pharmacological profile. Journal of Pharmacology and Experimental Therapeutics 241, 117-124 (1987).
| Cas No. | 101910-24-1 | SDF | |
| 化学名 | α-pentyl-3-(2-quinolinylmethoxy)-benzenemethanol | ||
| Canonical SMILES | CCCCCC(O)c1cccc(OCc2ccc3ccccc3n2)c1 | ||
| 分子式 | C22H25NO2 | 分子量 | 335.4 |
| 溶解度 | ≤100mg/ml in ethanol;100mg/ml in methanol;100mg/ml in acetone;100mg/ml in DMSO;100mg/ml in etonitrile. | 储存条件 | Room temperature |
| 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 | 2.9815 mL | 14.9076 mL | 29.8151 mL |
| 5 mM | 0.5963 mL | 2.9815 mL | 5.963 mL |
| 10 mM | 0.2982 mL | 1.4908 mL | 2.9815 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。