Tibenelast sodium (LY 186655)
(Synonyms: LY 186655) 目录号 : GC31823
Tibenelast sodium (LY 186655) 是一种磷酸二酯酶抑制剂。
Cas No.:105102-18-9
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Tibenelast sodium is a phosphodiesterase inhibitor.
The effect of the phosphodiesterase inhibitor Tibenelast, and placebo on isoproterenol-induced changes in heart rate, cAMP and norepinephrine levels in normal male volunteers is studied. Tibenelast increases the heart rate response to isoproterenol infusion, whereas norepinephrine and cAMP levels are not different in any treatment[1].
Tibenelast is a potent orally active compound against anaphylactic shock induced by high dose antigen aerosol. When a lower aerosol challenge (0.05 mg/mL) is employed, bronchoconstriction is observed with a concomitant increase in lung resistance (RL) and a fall in dynamic compliance (Cdyn). Tibenelast at 25 mg/kg p.o. prevents these changes. Tibenelast is 10 times more potent than Aminophylline by i.v. administration; normalization of pulmonary function is achieved at 1 mg/kg i.v. Tibenelast is synergistic with epinephrine. The oral dose response curve of Tibenelast is enhanced with the co-administration of epinephrine. Tibenelast may be of significant value in the treatment of asthma and other respiratory diseases[2].
[1]. Schwertschlag US, et al. Effect of tibenelast (a phosphodiesterase inhibitor) and theophylline on isoproterenol-stimulated heart rate, cyclic AMP and norepinephrine levels. Pharmacology. 1993;46(3):142-7. [2]. Ho PP, et al. Tibenelast, 5,6-diethoxybenzo(B)thiophene-2-carboxylic acid, sodium salt (LY186655), is an orally active anti-asthma compound in the guinea pig. Life Sci. 1990;46(13):917-25.
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.4687 mL | 17.3436 mL | 34.6873 mL |
| 5 mM | 0.6937 mL | 3.4687 mL | 6.9375 mL |
| 10 mM | 0.3469 mL | 1.7344 mL | 3.4687 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。