Isosorbide Dinitrate
(Synonyms: 硝酸异山梨酯; ISDN) 目录号 : GC45488
A nitric oxide donor
Cas No.:87-33-2
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
Isosorbide dinitrate is an organic nitrate ester and nitric oxide (NO) donor in the same class as nitroglycerin.1 It induces vasodilation with IC50 values of 0.56 and 1.82 μM for isolated precontracted rabbit femoral vein and artery, respectively.2 Isosorbide dinitrate increases oxygenation of tumor tissue in vivo in a mouse xenograft model.3 It also inhibits platelet aggregation in vitro and in vivo at concentrations in the micromolar range.4 Formulations containing isosorbide dinitrate have been used for the treatment of angina pectoris.
References
1. Ahlner, J., Andersson, R.G., Torfgard, K., et al. Organic nitrate esters: Clinical use and mechanisms of actions. Pharmacol. Rev. 43(3), 351-423 (1991).
2. Toyoda, J., Hisayama, T., and Takayanagi, I. Nitro compounds (isosorbide dinitrate, 5-isosorbide mononitrate and glyceryl trinitrate) on the femoral vein and femoral artery. Gen. Pharmacol. 17(1), 89-91 (1986).
3. Jordan, B.F., Misson, P., Demeure, R., et al. Changes in tumor oxygenation/perfusion induced by the no donor, isosorbide dinitrate, in comparison with carbogen: Monitoring by EPR and MRI. Int. J. Radiat. Oncol. Biol. Phys. 48(2), 565-570 (2000).
4. De Caterina, R., Giannessi, D., Bernini, W., et al. Organic nitrates: Direct antiplatelet effects and synergism with prostacyclin. Antiplatelet effects of organic nitrates. Thromb. Haemost. 59(2), 207-211 (1988).
| Cas No. | 87-33-2 | SDF | |
| 别名 | 硝酸异山梨酯; ISDN | ||
| Canonical SMILES | [H][C@@]1([C@@H](O[N+]([O-])=O)CO2)[C@@]2([H])[C@H](O[N+]([O-])=O)CO1 | ||
| 分子式 | C6H8N2O8 | 分子量 | 236.1 |
| 溶解度 | Chloroform: Slightly Soluble,Methanol: Slightly Soluble | 储存条件 | 4°C, protect from light |
| 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 | 4.2355 mL | 21.1775 mL | 42.3549 mL |
| 5 mM | 0.8471 mL | 4.2355 mL | 8.471 mL |
| 10 mM | 0.4235 mL | 2.1177 mL | 4.2355 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。
Pharmacokinetics of Isosorbide Dinitrate and isosorbide-5-mononitrate
Int J Clin Pharmacol Ther Toxicol 1989 Sep;27(9):445-53.PMID:2681004doi
Short-acting nitrates like glyceryl trinitrate are most suitable for interrupting attacks of angina pectoris, long-acting nitrates for their prophylaxis. A salient feature of drugs used in prophylaxis is a long duration of action. Among many organic nitrates developed for this purpose, ISDN became the most prominent. ISDN is metabolized to isosorbide-2-mononitrate (IS-2-MN) and isosorbide-5-mononitrate (IS-5-MN) which are pharmacologically active. Since denitration is practically the only way of elimination, the denitration rate of the compounds is proportional to their total body clearance, which is 3.2 l/min for ISDN, 0.371 l/min for IS-2-MN and 0.124 l/min for IS-5-MN. Their terminal elimination half-life is 63, 108 and 264 min respectively. These figures are the weighted means from studies with intravenous administration. Several authors determined the AUCs of ISDN and its mononitrates after administration of ISDN. From the AUCs and the respective total body clearances, the amounts of ISDN were calculated which enter the systemic circulation intact, and those of the mononitrates formed by denitration of ISDN. After intravenous administration of ISDN, 62% were metabolized to IS-5-MN, 24% to IS-2-MN. The remaining 14% must be eliminated by other routes. After oral administration as plain tablets, 26% of the ISDN enter the systemic circulation intact. Forty-seven percent of the dose are metabolized to IS-5-MN during absorption, 17% after absorption. The figures for IS-2-MN are 14% and 5%, respectively.(ABSTRACT TRUNCATED AT 250 WORDS)
BiDil (Isosorbide Dinitrate and hydralazine): a new fixed-dose combination of two older medications for the treatment of heart failure in black patients
Cardiol Rev 2007 Jan-Feb;15(1):46-53.PMID:17172884DOI:10.1097/01.crd.0000250840.15645.fb.
BiDil is a new fixed-dose combination of 2 older medications, Isosorbide Dinitrate (ISDN) and hydralazine. ISDN is an organic nitrate that is biotransformed into nitric oxide, a potent vasodilator. Hydralazine is believed to have both vasodilatory properties specific to the arteries and antioxidant properties, which address both the biochemical alterations in the failing cardiovascular system as well as the issue of nitrate tolerance. A drug regimen combining an NO stimulator (ISDN) with an antioxidant (hydralazine) favorably influences the nitroso-redox balance. Retrospective analyses of previous heart failure (HF) clinical trials comparing the combination of ISDN and hydralazine with placebo and enalapril, respectively, demonstrated a benefit in the black population, setting the precedent for a race-based therapeutic study, the African-American Heart Failure Trial (A-HeFT). A-HeFT examined the use of BiDil added to standard HF therapy in blacks with New York Heart Association functional class III and IV HF. BiDil demonstrated a 43% reduction in mortality when compared with placebo. As a result, current evidence-based treatment guidelines recommend that the addition of ISDN and hydralazine in black patients with moderate to severe HF optimized on standard therapy be considered. BiDil is currently indicated for the treatment of HF as an adjunct to standard therapy in black patients. The use of BiDil for black patients with mild disease or in nonblack patients with HF has not been studied. Future clinical trials involving an ethnically and clinically diverse population of patients would further define the role of combined ISDN and hydralazine in the treatment of HF.
Comparative effects of nitroglycerin and Isosorbide Dinitrate on coronary collateral vessels and ischemic myocardium in dogs
Am J Cardiol 1976 Feb;37(2):244-9.PMID:813510DOI:10.1016/0002-9149(76)90319-2.
To determine the effect of Isosorbide Dinitrate or ischemic myocardium, this agent was administered to dogs with well developed coronary collateral vessels 8 to 14 weeks after embolization and subsequent occlusion of the left anterior descending coronary artery. After thoracotomy the left coronary artery was cannulated and perfused with blood from the femoral artery. The distal left anterior descending artery was cannulated to monitor peripheral coronary pressure. Regional contractile force in the normal left circumflex and potentially ischemic left anterior descending regions was measured with isometric strain gauge arches sewn to the epicardium. Moderate decreases in coronary perfusion pressure averaging 27 mm Hg produced selective ischemia in the myocardium beyond the site of occlusion of the left anterior descending artery. Under these conditions the average increase in peripheral coronary pressure produced by intracoronary injection of Isosorbide Dinitrate was 9.0 mm Hg, whereas contractile force in the ischemic region increased by 30 percent. The contractile force was unchanged in the normal regions. Therefore, Isosorbide Dinitrate can dilate coronary collateral vessels and improve contractile force in ischemic areas. Intracoronary injection of nitroglycerin had similar effects. The durations of responses to Isosorbide Dinitrate and nitroglycerin were remarkably similar: 6.4 and 6.7 minutes, respectively. Although Isosorbide Dinitrate can directly dilate coronary collateral vessels, its effects are not longer lasting than those of nitroglycerin.
Role of Isosorbide Dinitrate in management of chronic congestive heart failure
Am Heart J 1985 Jul;110(1 Pt 2):264-8.PMID:3893081DOI:10.1016/0002-8703(85)90498-3.
Congestive heart failure is accompanied by a number of compensatory mechanisms that may overshoot the mark. Among these are excessive arteriolar and venous constriction. Nitrates are effective in producing venodilation, redistributing blood from the chest to the periphery, and lowering right and left atrial pressures. Although oral Isosorbide Dinitrate is effective in producing acute beneficial hemodynamic effects, it usually does not increase exercise tolerance in the short term. Prolonged administration, however, does increase exercise tolerance and improve clinical class. Isosorbide Dinitrate can be effectively combined with an arteriolar dilator such as hydralazine, which increases cardiac output. Such vasodilator therapy is symptomatically effective in patients with heart failure, although there is no evidence to date to suggest a prolongation of life.
The role of Isosorbide Dinitrate in the treatment of perioperative hypertension
Am Heart J 1985 Jul;110(1 Pt 2):273-6.PMID:3925746DOI:10.1016/0002-8703(85)90500-9.
Intravenous nitroglycerin (NTG) has recently been found to be useful for the control of blood pressure during the perioperative period, especially during coronary artery bypass procedures. The objective of this study was to determine whether intravenous Isosorbide Dinitrate (ISDN) could play a similar role. Sixty-seven patients undergoing coronary artery bypass grafting at three centers were randomly assigned to an ISDN or NTG treatment group. The hemodynamic performance of all patients was assessed by the methods commonly used for cardiac patients (ECG, arterial line, thermodilution pulmonary artery catheter). One of the two nitrates was infused whenever the systolic blood pressure or the pulmonary capillary wedge pressure exceeded predetermined values. Treatment by either agent was considered successful if the elevated values returned to normal. NTG reduced the blood pressure in a higher percentage of hypertensive events. The rates of success were 84% for NTG vs 72% for ISDN in the prebypass phase, 93% vs 64% in the postbypass phase, and 71% vs 54% in the postoperative phase. Increased ISDN effectiveness may be attained with the use of a bolus administration before continuous infusion or with the use of a rapid rate of infusion.