L-NAME HCl

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 K_i of 15 nM, 39 nM and 4.4 μM, respectively.

CAS No. 51298-62-5

サイズ	価格(税別)	在庫状況
100mg	JPY 22000	国内在庫あり
1g	JPY 55500	国内在庫なし(納期7~10日)

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文献中Selleckの製品使用例（37）

製品安全説明書

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L-NAME HCl関連製品

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NOS阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	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 K_i 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
Kinase 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.

参考
[1] Furfine ES, et al. Biochemistry, 1993, 32(33), 8512-8517. [2] Rees DD, et al. Br J Pharmacol, 1990, 101(3), 746-752. [3] Du Y, et al. J Physiol Regul Integr Comp Physiol, 2004, 287(4), R735-R741. [4] Heggers JP, et al. J Altern Complement Med, 1997, 3(2), 149-153. + 展開

参考

[4] Heggers JP, et al. J Altern Complement Med, 1997, 3(2), 149-153.

+ 展開

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	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

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
=	×	×

希釈計算器分子量計算器

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）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

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。

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):