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L-NAME HCl NOS inhibitor

Cat. No.: S2877

L-NAME HCl (NG-Nitroarginine methyl ester, N-Nitro-L-arginine methylester) is a nonselective inhibitor of nitric oxide synthetases (NOS) for nNOS (bovine), eNOS (human), and iNOS (murine), with Ki of 15 nM, 39 nM and 4.4 μM, respectively. This compound can be used to induce animal models of Hypertension.
L-NAME HCl NOS inhibitor Chemical Structure

Estructura química

Peso molecular: 269.69

Saltar a

Control de calidad (Quality Control)

Lote: Pureza: 99.94%
99.94

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Líneas celulares Tipo de ensayo Concentración Tiempo de incubación Formulación Descripción de la actividad PMID
mouse BV2 cells Function assay 24 h Inhibition of Nitric oxide synthase activity in mouse BV2 cells assessed as LPS-induced NO production after 24 hrs by Griess reaction, IC50=18.9 μM 21377368
mouse RAW264.7 cells Function assay 17-20 h Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFN-gamma/LPS-stimulated nitric oxide production after 17 to 20 hrs by Griess assay, IC50=27.13 μM 19359068
HUVEC Function assay Ability to inhibit conversion of [3H]L-Arg to [3H]L-citrulline catalyzed by endothelial NOS (e NOS) from HUVEC cells, IC50=2.7μM 11327580
DLD-1 Function assay Ability to inhibit conversion of [3H]L-Arg to [3H]L-citrulline catalyzed by inducible NOS (i NOS) from human DLD-1 cells, IC50=14μM 11327580
BV2 Function assay Inhibition of NOS-dependent nitric oxide production in mouse BV2 cells, IC50=36μM 17046255
BV2 Function assay Inhibition of nitric oxide synthase in mouse BV2 cells assessed as inhibition of LPS-induced NO production, IC50=20.1μM 18161942
BV2 Function assay Inhibition of iNOS-mediated NO production in LPS-induced mouse BV2 cells, IC50=25.8μM 18926710
BV2 Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced iNOS-dependent nitrite production after 24 hrs by Griess method, IC50=25.8μM 21028898
BV2 Function assay Inhibition of iNOS in mouse BV2 microglial cells assessed as NO production, IC50=25.8μM 21115251
RAW264.7 Function assay 1 hr Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells preincubated with compound for 1 hr before exposure to LPS measured after 24 hrs by Griess reaction method, IC50=48.5μM 21435874
Sf9 Function assay 45 mins 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, IC50=0.68μM 21923116
Sf9 Function assay 45 mins 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, IC50=0.69μM 21923116
Sf9 Function assay 45 mins 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, IC50=0.83μM 21923116
BV2 Function assay 24 hrs Inhibition of iNOS-mediated nitric oxide production in LPS-stimulated mouse BV2 cells measured after 24 hrs of post-stimulation by Griess reaction method, IC50=13.35μM 22115618
BV2 Function assay 1 hr Inhibition of LPS-induced NO production in mouse BV2 cells preincubated for 1 hr followed by LPS addition measured after 24 hrs by Griess assay, IC50=24.7μM 27588326
RAW264.7 Antiinflammatory assay 2 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production preincubated for 2 hrs followed by LPS stimulation measured after 18 hrs by Griess assay, IC50=30.6μM 28099011
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
RAW264.7 Anti-inflammatory assay 17 to 20 hr Anti-inflammatory activity in Mus musculus (mouse) RAW264.7 cells assessed as inhibition of IFN-gamma/LPS-induced NO production after 17 to 20 hr by Griess assay, IC50=23.21μM ChEMBL
RAW264.7 Anti-inflammatory assay 17 to 20 hr Anti-inflammatory activity in Mus musculus (mouse) RAW264.7 cells assessed as inhibition of IFN-gamma/LPS-induced nitric oxide production after 17 to 20 hr by Griess assay, IC50=26.21μM ChEMBL
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Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular 269.69 Fórmula

C7H15N5O4.HCl

 Almacenamiento (Desde la fecha de recepción)
Nº CAS 51298-62-5 Descargar SDF Almacenamiento de soluciones madre

Sinónimos NG-Nitroarginine methyl ester, N-Nitro-L-arginine methylester Smiles COC(=O)C(CCCN=C(N)N[N+](=O)[O-])N.Cl

Solubilidad (Solubility)

In vitro
Lote:

Water : 54 mg/mL

DMSO : Insoluble
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Ethanol : Insoluble

Calculadora de Molaridad

Masa Concentración Volumen Peso molecular
Calculadora de Dilución Calculadora de Peso Molecular

In vivo
Lote:

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

mg/kg g μL

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH2O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción (Mechanism of Action)

Targets/IC50/Ki
nNOS
(Cell-free assay)
15 nM(Ki)
eNOS
(Cell-free assay)
39 nM(Ki)
In vitro
NG-nitro-L-arginine methyl ester (L-NAME; at 0.1-100 mM) causes concentration-dependent inhibition of the Ca2(+)-dependent endothelial NO synthase from porcine aortae. This compound causes an endothelium-dependent contraction and an inhibition of the endothelium-dependent relaxation induced by acetylcholine (ACh) in aortic rings. In another research, Viability of rMC-1 cells or BREC in 25 mM glucose is significantly less than at 5 mM glucose, and this cell death is inhibited by this chemical in both cell types.
Ensayo de quinasa
Ensayo enzimático
La oxidación de L-NAME HCl (clorhidrato de éster metílico de Nω-nitro-L-arginina) se monitoriza mediante la conversión de [3H]- o [14C]-arginina a L-citrulina, que separa la L-citrulina de la L-arginina mediante cromatografía Dowex 50x8-200 (Na). Las mezclas de reacción típicas (100 pL) contienen 50 mM HEPES, pH 7,0, 8 pM tetrahidrobiopterina, 1 mM CaC12, 0,01 mg/mL calmodulina, 0,5 mM EDTA, 0,450 pM [14C]-arginina (30000 cpm) y 100-200 pM NADPH. La oxidación de NADPH a NADP+ catalizada por la cNOS se monitoriza mediante la reducción de la absorbancia a 340 nm con un espectrofotómetro Kontron 860 en un volumen de 300 pL. Todas las reacciones se realizan a 30 ℃ a menos que se indique lo contrario.
In vivo
L-NAME HCl (0.03-300 mg kg-1, i.v.) induces a dose-dependent increase in mean systemic arterial blood pressure accompanied by bradycardia. This compound (100 mg kg-1, i.v.) inhibits significantly the hypotensive responses to ACh and bradykinin. The increase in blood pressure and bradycardia produced by this chemical is reversed by L-arginine (30-100 mg kg-1, i.v.) in a dose-dependent manner.
Referencias
  • [4] https://pubmed.ncbi.nlm.nih.gov/9395704/