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L-NAME hydrochloride

Catalog No.
A7088
NO synthase inhibitor
Grouped product items
SizePriceStock Qty
100mg
$55.00
In stock
500mg
$77.00
In stock
1g
$99.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

L-NAME Hydrochloride is an inhibitor of nitric oxide synthase (NOS) with IC50 value of 70 μM [1].?

NOS is an important enzyme involved in production of NO. NO, the smallest signaling molecule known, controls servoregulatory functions such as neurotransmission or vascular tone, regulates gene transcription and mRNA translation, as well as produces post-translational modifications of proteins [2].?

At concentrations of 10-9 ~ 10-3 M, L-NAME Hydrochloride inhibited NOS purified from rat brains in a dose dependent manner, with IC50 value of 70 μM [1]. In another study, L-NAME Hydrochloride at 0.1 ~ 100 mM caused concentration-dependent inhibition of the Ca2+-dependent endothelial NO synthase from porcine aortae. L-NAME Hydrochloride also caused an endothelium-dependent contraction and an inhibition of the endothelium-dependent relaxation induced by acetylcholine (ACh) in aortic rings [3].?

In anaesthetized rats, L-NAME Hydrochloride (0.03 ~ 300 mg/kg, i.v.) induced a dose-dependent increase in mean systemic arterial blood pressure accompanied by bradycardia. L-NAME Hydrochloride (100 mg/kg, i.v.) significantly inhibited the hypotensive responses to ACh and bradykinin. The increase in blood pressure and bradycardia produced by L-NAME Hydrochloride could be reversed by L-arginine (30 ~ 100 mg/kg, i.v.) in a dose-dependent manner [3].?

References:

[1]. Pfeiffer S, Leopold E, Schmidt K, et al. Inhibition of nitric oxide synthesis by NG-nitro-L-arginine methyl ester (L-NAME): requirement for bioactivation to the free acid, NG-nitro-L-arginine. British Journal of Pharmacology, 1996, 118(6): 1433-1440.

[2]. F?rstermann U, Sessa W C. Nitric oxide synthases: regulation and function. European Heart Journal, 2012, 33(7): 829-837.

[3]. Rees D D, Palmer R M, Schulz R, et al. Characterization of three inhibitors of endothelial nitric oxide synthase in vitro and in vivo. British Journal of Pharmacology, 1990, 101(3): 746-752.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt269.7
Cas No.51298-62-5
FormulaC7H15N5O4·HCl
SynonymsL-NAME, L-NAME HCL
Solubility≥27 mg/mL in H2O; insoluble in EtOH; ≥23 mg/mL in DMSO
Chemical Namemethyl (2S)-2-amino-5-[[amino(nitramido)methylidene]amino]pentanoate;hydrochloride
SDFDownload SDF
Canonical SMILESCOC(=O)C(CCCN=C(N)N[N+](=O)[O-])N.Cl
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment:[1]

Cell lines

Bovine retinal endothelial cells (BRECs) and rat retinal müller cell line rMC-1

Reaction Conditions

1 mM L-NAME for 5 d incubation

Applications

L-NAME inhibited production of NO and prostaglandin E2 as well as expression of iNOS and COX-2 in rMC-1 cells exposed to 25 mM glucose. Moreover, L-NAME also reduced BREC and rMC-1 cell death in the high glucose condition.
Animal experiment:[2]

Animal models

Male Wistar rats, 200 ~ 300 g

Dosage form

0.03 ~ 300 mg/kg

Intravenous administration (i.v.)

Applications

L-NAME (0.03 ~ 300 mg/kg, i.v.) induced a dose-dependent increase in mean systemic arterial blood pressure accompanied by bradycardia. Furthermore, L-NAME (100 mg/kg, i.v.) inhibited significantly the hypotensive responses to acetylcholine and bradykinin. The increases in blood pressure and bradycardia produced by L-NAME were reversed by L-arginine (30 ~ 100 mg/kg, i.v.) in a dose-dependent manner. Therefore, L-NAME could be used to study the important role of NO synthesis in the maintenance of vascular tone and blood pressure.

Note

The technical data provided above is for reference only.

References:

1. Du Y, Sarthy VP, Kern TS. Interaction between NO and COX pathways in retinal cells exposed to elevated glucose and retina of diabetic rats. American Journal of Physiology-Regulatory, Integrative and Comparative Physiology, 2004, 287(4): R735-741.

2. Rees DD, Palmer RM, Schulz R, et al. Characterization of three inhibitors of endothelial nitric oxide synthase in vitro and in vivo. British Journal of Pharmacology, 1990, 101(3): 746-752.

Biological Activity

Description L-NAME hydrochloride is a NO synthase inhibitor.
Targets            
IC50            

Quality Control