ICI 153110
目录号 : GC32643
ICI153110是一种口服有效的磷酸二酯酶抑制剂，具有血管舒张和收缩力性质，可用于治疗充血性心力衰竭。
Cas No.:87164-90-7
Sample solution is provided at 25 µL, 10mM.
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ICI 153110 is an orally active phosphodiesterase inhibitor with both vasodilating and inotropic properties which is designed for the treatment of congestive cardiac failure.
ICI 153110 is an orally active phosphodiesterase inhibitor with both vasodilating and inotropic properties which is designed for the treatment of congestive cardiac failure. Fourteen animals have died as a direct or indirect consequence of ICI 153110 administration in the high-dose main test and reversibility groups. In the female rat dosed at 10 mg/kg/day ICI 153110 a mild focal arteritis is characterized by a predominantly and diffusely adventitial infiltration of mixed cells and early formation of fibrous tissue. The two rats dosed at 250 mg/kg/day ICI 153110 die prematurely from intratracheal intubation of dosing solution. Arteries from two further animals (dosed at 5 and 250 mg/kg/day ICI 153110) show minimal focal arteritis with medial necrosis, and medial and adventitial inflammation[1].
[1]. Westwood FR, et al. Pathologic changes in blood vessels following administration of an inotropic vasodilator (ICI 153,110) to the rat. Fundam Appl Toxicol. 1990 May;14(4):797-809.
Animal experiment: | Alderley Park APfSD rats are used in this study. In all, 150 male rats and 150 female rats are assigned to four groups (one control and three treatment) in the two separate studies; 30 per sex representing the main (regular) test groups and 15 per sex for investigating reversibility of effects following treatment at the highest dose employed (withdrawal studies). The dose levels are 5, 10, and 250 mg/kg/day of ICI 153110. All animals are dosed orally, by gavage, using a plastic syringe and a flexible catheter. Equal numbers of animals per sex in the four groups are necropsied necropsied at each of two time points; following at least 28 consecutive days dosing (1 month) and 182 consecutive days of dosing (6 months). All animals are observed at least twice daily for any abnormal signs, all of which are recorded. Body weights, food consumption, water consumption, clinical pathology, and pharmacokinetics are also measured[1]. |
References: [1]. Westwood FR, et al. Pathologic changes in blood vessels following administration of an inotropic vasodilator (ICI 153,110) to the rat. Fundam Appl Toxicol. 1990 May;14(4):797-809. | |
| Cas No. | 87164-90-7 | SDF | |
| Canonical SMILES | O=C1CCC(/C=C/C2=CC=NC=C2)=NN1 | ||
| 分子式 | C11H11N3O | 分子量 | 201.22 |
| 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 | 4.9697 mL | 24.8484 mL | 49.6968 mL |
| 5 mM | 0.9939 mL | 4.9697 mL | 9.9394 mL |
| 10 mM | 0.497 mL | 2.4848 mL | 4.9697 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet