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NCX899

Katalog-Nr.GC32560 Copy One-Click Copy Product Info

NCX899 ist ein NO-freisetzendes Derivat von Enalapril und zeigt eine hemmende AktivitÄt gegen die AktivitÄt des Angiotensin-Converting-Enzyms (ACE).

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NCX899 Chemische Struktur

Cas No.: 690655-41-5

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1mg
368,00 $
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5mg
735,00 $
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10mg
1.250,00 $
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20mg
2.206,00 $
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Sample solution is provided at 25 µL, 10mM.



Description of NCX899

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.

Protocol of NCX899

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.

Chemical Properties of NCX899

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
Formula C23H33N3O8 M.Wt 479.52
Löslichkeit 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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of NCX899

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.0854 mL 10.4271 mL 20.8542 mL
5 mM 417.1 μL 2.0854 mL 4.1708 mL
10 mM 208.5 μL 1.0427 mL 2.0854 mL
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In vivo Formulation Calculator (Clear solution) of NCX899

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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.

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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 39 reference(s) in Google Scholar.)

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