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L-NAME HCl

別名：NG-Nitroarginine methyl ester, N-Nitro-L-arginine methylester

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.

L-NAME HCl化学構造

CAS No. 51298-62-5

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代表番号: 045-509-1970|電子メール：[email protected]
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L-NAME HCl関連製品

NOS阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
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
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
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
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
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
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 Function assay Inhibition of iNOS in mouse BV2 microglial cells assessed as NO production, IC50=25.8μM 21115251
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
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生物活性

製品説明 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.
Targets
nNOS [1]
(Cell-free assay)		 eNOS [1]
(Cell-free assay)
15 nM(Ki) 39 nM(Ki)
In Vitro
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. L-NAME causes an endothelium-dependent contraction and an inhibition of the endothelium-dependent relaxation induced by acetylcholine (ACh) in aortic rings. [2] 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 l-NAME in both cell types. [3]
Kinase Assay Enzyme Assay
The oxidation of L-arginine is monitored by the conversion of [3H]- or [14C]-arginine to L-citrulline which separates L-citrulline from L-arginine by Dowex 50x8-200 (Na) chromatography. Typical reaction mixtures (100 pL) contains 50 mM HEPES, pH 7.0, 8 pM tetrahydrobiopterin, 1 mM CaC12, 0.01 mg/mL calmodulin, 0.5 mM EDTA, 0.450 pM [14C]-arginine (30000 cpm), and 100-200 pM NADPH. The cNOS-catalyzed oxidation of NADPH to NADP+ is monitored by the reduction of absorbance at 340 nm with a Kontron 860 spectrophotometer in a volume of 300 pL. All reactions are at 30 ℃ unless otherwise indicated.
細胞実験 細胞株 rMC-1 cells
濃度 1 mM
反応時間 5 days
実験の流れ rMC-1 cells are incubated in 5 or 25 mM glucose, with or without l-NAME (1 mM). Media is changed every other day for up to 5 days. BREC cells are incubated in 5 or 25 mM glucose as well as inhibitor as described above for 5 days. Cell death is determined by light microscopy using a hemocytometer and a 0.4% trypan blue dye exclusion method. The number of cells that do not exclude the dye is expressed per 1,000 total cells. A minimum of 800 cells is counted per assay (8 dishes, >100 cells counted per dish), and the assay is replicated three times on different days.
In Vivo
In Vivo L-NAME (0.03-300 mg kg-1, i.v.) induces a dose-dependent increase in mean systemic arterial blood pressure accompanied by bradycardia. L-NAME (100 mg kg-1, i.v.) inhibits significantly the hypotensive responses to ACh and bradykinin. The increase in blood pressure and bradycardia produced by L-NAME is reversed by L-arginine (30-100 mg kg-1, i.v.) in a dose-dependent manner. [2]
動物実験 動物モデル Male Wistar rats
投与量 100 mg/kg
投与経路 i.v.

化学情報

分子量 269.69 化学式

C7H15N5O4.HCl
CAS No. 51298-62-5 SDF Download L-NAME HCl SDFをダウンロードする
Smiles COC(=O)C(CCCN=C(N)N[N+](=O)[O-])N.Cl
保管

In vitro
Batch:

Water : 54 mg/mL

DMSO : Insoluble ( 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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