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L-NAME HCl NOS Remmer

Cat.nr.: S2877

L-NAME HCl (NG-Nitroarginine methyl ester, N-Nitro-L-arginine methylester) is een niet-selectieve remmer van nitric oxide synthetases (NOS) voor nNOS (rund), eNOS (mens) en iNOS (muis), met een Ki van respectievelijk 15 nM, 39 nM en 4,4 μM. Deze verbinding kan worden gebruikt om diermodellen van hypertensie te induceren.
L-NAME HCl NOS Remmer Chemical Structure

Chemische structuur

Molecuulgewicht: 269.69

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.94%
99.94

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen Assaytype Concentratie Incubatietijd Formulering Activiteitsbeschrijving 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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Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Molecuulgewicht 269.69 Formule

C7H15N5O4.HCl

 Opslag (vanaf de datum van ontvangst)
CAS-nr. 51298-62-5 SDF downloaden Opslag van stamoplossingen

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

Oplosbaarheid (Solubility)

In vitro
Batch:

Water : 54 mg/mL

DMSO : Insoluble
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : Insoluble

Molariteitscalculator

Massa Concentratie Volume Molecuulgewicht
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In vivo
Batch:

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

mg/kg g μL

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH2O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (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.
Kinase Assay
Enzymtest
De oxidatie van L-NAME HCl (Nω-nitro-L-arginine methylesterhydrochloride) wordt gemonitord door de omzetting van [3H]- of [14C]-arginine naar L-citrulline, dat L-citrulline scheidt van L-arginine door Dowex 50x8-200 (Na) chromatografie. Typische reactiemengsels (100 pL) bevatten 50 mM HEPES, pH 7,0, 8 pM tetrahydrobiopterine, 1 mM CaC12, 0,01 mg/mL calmoduline, 0,5 mM EDTA, 0,450 pM [14C]-arginine (30000 cpm), en 100-200 pM NADPH. De cNOS-gekatalyseerde oxidatie van NADPH naar NADP+ wordt gemonitord door de reductie van de absorptie bij 340 nm met een Kontron 860 spectrofotometer in een volume van 300 pL. Alle reacties zijn bij 30 ℃ tenzij anders aangegeven.
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.
Referenties
  • [4] https://pubmed.ncbi.nlm.nih.gov/9395704/