L-NAME (hydrochloride) [51298-62-5]

Minimum order 2

Cat# HY-18729A-100mg

Size : 100mg

Brand : MedChemExpress


Description

L-NAME hydrochloride inhibits NOS with an IC50 of 70 μM. L-NAME is a precursor to NOS inhibitor L-NOARG which has an IC50 value of 1.4 μM. L-NAME hydrochloride requires hydrolysis of the methyl ester by cellular esterases to become a fully functional inhibitor. L-NAME hydrochloride can be used to induce hypertension and preeclampsia models.

IC50 & Target

IC50: 70 μM (NOS)[1]

Cellular Effect
Cell Line Type Value Description References
Sf9 IC50
0.68 μM
Compound: L-NAME
Inhibition of human recombinant eNOS expressed in Sf9 cells assessed as inhibition of conversion of [3H]-L-arginine to [3H]-L-citrulline after 45 mins by liquid scintillation counting
Inhibition of human recombinant eNOS expressed in Sf9 cells assessed as inhibition of conversion of [3H]-L-arginine to [3H]-L-citrulline after 45 mins by liquid scintillation counting
[PMID: 21923116]
Sf9 IC50
0.69 μM
Compound: L-NAME
Inhibition of human recombinant nNOS expressed in Sf9 cells assessed as inhibition of conversion of [3H]-L-arginine to [3H]-L-citrulline after 45 mins by liquid scintillation counting
Inhibition of human recombinant nNOS expressed in Sf9 cells assessed as inhibition of conversion of [3H]-L-arginine to [3H]-L-citrulline after 45 mins by liquid scintillation counting
[PMID: 21923116]
Sf9 IC50
0.83 μM
Compound: L-NAME
Inhibition of human recombinant iNOS expressed in Sf9 cells assessed as inhibition of conversion of [3H]-L-arginine to [3H]-L-citrulline after 45 mins by liquid scintillation counting
Inhibition of human recombinant iNOS expressed in Sf9 cells assessed as inhibition of conversion of [3H]-L-arginine to [3H]-L-citrulline after 45 mins by liquid scintillation counting
[PMID: 21923116]
In Vitro

L-arginine analogues are widely used inhibitors of nitric oxide synthase (NOS) activity, with Nw-nitro-L-arginine methyl ester (L-NAME) being at the head[2]. Freshly dissolved L-NAME is a 50 fold less potent inhibitor of purified brain NOS (mean IC50= 70 μM) than L-NOARG (IC50= 1.4 μM), but the apparent inhibitory potency of L-NAME approached that of L-NOARG upon prolonged incubation at neutral or alkaline pH. HPLC analyses reveal that NOS inhibition by L-NAME closely correlated with hydrolysis of the drug to L-NOARG[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Note:
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

L-NAME hydrochloride can be used to induce hypertension models[6].

Induction of hypertension Model[6]
Background
L-NAME hydrochloride decreases nitric oxide (NO) release with an inhibition competence in endothelial nitric oxide synthase (eNOS) in animals.
Specific Modeling Methods
Mice: Swiss Webster • male • 6-week-old
Administration: 400 mg/kg • ip • once daily for 7 days
Modeling Indicators
Body quality changes: Induced hypertension with body weight loss and high blood pressure.

2. Induction of preeclampsia[8]
Background
L-NAME induces preeclampsia by reducing the production of nitric oxide through inhibiting nitric oxide synthase, triggering a series of changes such as vasoconstriction, placental dysfunction, inflammatory response, and anti-angiogenesis.
Specific Modeling Methods
Mice: CBA x C57BL/6 pregnant female mice • 6-16 weeks old
Administration: subcutaneous injection • 50 mg/kg/day • E7.5 to E17.5
Modeling Indicators
Elevated blood pressure, impaired fetal and placental growth, and increased circulating endothelin-1 (vasoconstrictor), soluble fms-like tyrosine kinase-1 (anti-angiogenic factor), and C-reactive protein (inflammatory marker).

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley (SD) rats [7]
Dosage: 40 mg/kg, 5 weeks
Administration: drinking water
Result: Induced hypertension with body weight loss and high blood pressure.
Clinical Trial
Molecular Weight

269.69

Formula

C7H16ClN5O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N[C@@H](CCCNC(N[N+]([O-])=O)=N)C(OC)=O.06Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (370.80 mM; Need ultrasonic)

DMSO : 100 mg/mL (370.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7080 mL 18.5398 mL 37.0796 mL
5 mM 0.7416 mL 3.7080 mL 7.4159 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 140 mg/mL (519.11 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

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