NCX899
目录号 : GC32560
NCX899是一种能够释放NO的enalapril的衍生物，能够抑制angiotensin-convertingenzyme(ACE)的活性。
Cas No.:690655-41-5
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
Animal experiment: | Enalapril (40 nmol/kg per min), NCX899 (35 nmol/kg per min) or sterile saline are infused at a flow rate of 0.5 mL/min over 15 min. Next, cumulative doses of NG-nitro-l-arginine methyl ester (l-NAME; 0.1-10 mg/kg) are injected during infusion of enalapril, NCX899 or saline infusion. The l-NAME is infused at a rate of 0.5 mL/min over 15 min for each dose. At the end of each infusion, the resulting haemodynamic changes are recorded. The total dose administered of NCX899 and enalapril throughout the protocols is 3.5 and 4.0 µmol/kg, respectively. The haemodynamic variables are measured before and after each l-NAME dose in all groups. The MABP and HR are displayed continuously on a computer monitor and are recorded on a printer coupled to this system. Measurements of the haemodynamic events are performed in triplicate for each time period. |
References: [1]. Iwanaga Y, et al. A nitric oxide-releasing derivative of enalapril, NCX 899, prevents progressive cardiac dysfunction and remodeling in hamsters with heart failure. FASEB J. 2004 Mar;18(3):587-8. Epub 2004 Jan 20. | |
NCX899 is a NO-releasing derivative of enalapril, and shows inhibitory activity against angiotensin-converting enzyme (ACE) activity.
NCX 899 (NCX, 25 mg/kg, n=10) decreases the end-diastolic dimension in cardiomyopathic (CM) with heart failure. NCX 899 inhibits ACE activity and increases the plasma nitrate levels in CM hamster[1]. NCX899 (4 micromol/kg, i.v.) inhibits the activity of serum angiotensin-converting enzyme in dogs. NCX899 significantly attenuates both arterial hypertension and bradycardia[2].
[1]. Iwanaga Y, et al. A nitric oxide-releasing derivative of enalapril, NCX 899, prevents progressive cardiac dysfunction and remodeling in hamsters with heart failure. FASEB J. 2004 Mar;18(3):587-8. Epub 2004 Jan 20. [2]. Okuyama CE, et al. Pharmacokinetics and pharmacodynamics of a nitric oxide-releasing derivative of enalapril in male beagles. Clin Exp Pharmacol Physiol. 2007 Apr;34(4):290-5.
| Cas No. | 690655-41-5 | SDF | |
| Canonical SMILES | O=C(OCCCO[N+]([O-])=O)[C@H]1N(C([C@H](C)N[C@H](C(OCC)=O)CCC2=CC=CC=C2)=O)CCC1 | ||
| 分子式 | C23H33N3O8 | 分子量 | 479.52 |
| 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 | 2.0854 mL | 10.4271 mL | 20.8542 mL |
| 5 mM | 0.4171 mL | 2.0854 mL | 4.1708 mL |
| 10 mM | 0.2085 mL | 1.0427 mL | 2.0854 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 and pharmacodynamics of a nitric oxide-releasing derivative of enalapril in male beagles
Clin Exp Pharmacol Physiol 2007 Apr;34(4):290-5.PMID:17324140DOI:10.1111/j.1440-1681.2007.04559.x.
1. Pharmacological compounds that release nitric oxide (NO) have been useful tools in the evaluation of the broad role of NO in physiopathology and therapeutics. The present study compared the pharmacokinetics and pharmacodynamics of enalapril and an NO-releasing enalapril molecule (NCX899) in conscious male beagles. The effects of both enalapril and NCX899 in the arterial hypertension and bradycardia induced by acute NO inhibition in anaesthetized dogs were also investigated. 2. Dogs received either NCX899 (4 micromol/kg, i.v.) or enalapril (4 micromol/kg, i.v.), after which plasma concentrations of the analytes and metabolites were quantified by liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS). 3. In the NCX899 group, the area under the time-course curve (AUC(0-24h)) was 29.18 +/- 4.72, 229.37 +/- 51.32 and 5159.23 +/- 514.88 microg.h/L for the analytes nitro-enalapril, enalapril and enalaprilat, respectively. In the enalapril group, the AUC(0-24h) was 704.53 +/- 158.86 and 4149.27 +/- 847.30 microg.h/L for the analytes enalapril and enalaprilat, respectively. Statistical analysis of data from both groups showed a significant difference for the analyte enalapril, but not for enalaprilat. Moreover, NCX899 and enalapril were equally effective in inhibiting the activity of serum angiotensin-converting enzyme. 4. In anaesthetized dogs, i.v. administration of the NO synthase (NOS) inhibitor N(G)-nitro-l-arginine methyl ester (l-NAME; 0.1-10 mg/kg) significantly elevated arterial blood pressure, with concomitant bradycardia. The compound NCX899 significantly attenuated both arterial hypertension and bradycardia, whereas enalapril had no significant effect. 5. In conclusion, the present results showed that the NO-releasing derivative of enalapril NCX899 presents a pharmacokinetic/pharmacodynamic relationship similar to its parent compound enalapril. Moreover, NCX899 (but not enalapril) was effective in protecting against the cardiovascular changes induced by acute NOS inhibition.