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NCX899 Sale

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。

NCX899 Chemical Structure

Cas No.:690655-41-5

规格 价格 库存 购买数量
1mg
¥3,570.00
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5mg
¥7,140.00
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10mg
¥12,138.00
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20mg
¥21,420.00
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Sample solution is provided at 25 µL, 10mM.

Description

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.

实验参考方法

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.
[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.

化学性质

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
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溶解性数据

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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
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