ICI 153110 |
رقم الكتالوجGC32643
One-Click Copy Product Info
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ICI 153110 هو مثبط نشط للفوسفوديستيراز عن طريق الفم مع كل من خصائص توسع الأوعية والتقلص العضلي المصمم لعلاج قصور القلب الاحتقاني
Products are for research use only. Not for human use. We do not sell to patients.
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 | ||
| Formula | C11H11N3O | M.Wt | 201.22 |
| الذوبان | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.9697 mL | 24.8484 mL | 49.6968 mL |
| 5 mM | 993.9 μL | 4.9697 mL | 9.9394 mL |
| 10 mM | 497 μL | 2.4848 mL | 4.9697 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)