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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)是一種無選擇性的一氧化氮合成酶抑制劑,對nNOS (牛源), eNOS (人源)和iNOS (鼠源)的Ki值分別為15nM, 39 nM和4.4 μM。

L-NAME HCl Chemical Structure

L-NAME HCl Chemical Structure

CAS: 51298-62-5

規(guī)格 價格 庫存 購買數(shù)量
100mg 647.01 現(xiàn)貨
1g 3030.3 現(xiàn)貨
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L-NAME HCl相關(guān)產(chǎn)品

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
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

產(chǎn)品描述 L-NAME HCl (NG-Nitroarginine methyl ester, N-Nitro-L-arginine methylester)是一種無選擇性的一氧化氮合成酶抑制劑,對nNOS (牛源), eNOS (人源)和iNOS (鼠源)的Ki值分別為15nM, 39 nM和4.4 μM。
靶點
nNOS [1]
(Cell-free assay)
eNOS [1]
(Cell-free assay)
15 nM(Ki) 39 nM(Ki)
體外研究(In Vitro)
體外研究活性 NG-硝基-L-精氨酸甲酯(L-NAME; 0.1-100 mM)濃度依賴性抑制豬主動脈中Ca2(+)-依賴性內(nèi)皮NO合酶。L-NAME引起主動脈環(huán)中內(nèi)皮細胞依賴性收縮,以及乙酰膽堿(ACh)誘導的血管內(nèi)皮依賴性舒張反應(yīng)的抑制。[2]在另一項研究中,rMC-1細胞或BREC在25 mM葡萄糖中的活性顯著比在5 mM葡萄糖中低,這種細胞死亡在兩種細胞類型中被l-NAME抑制。[3]
激酶實驗 酶測定
L-精氨酸的氧化通過[3H]-或[14C]-精氨酸轉(zhuǎn)化為L-瓜氨酸監(jiān)測,通過Dowex 50x8-200 (Na)色譜分析從L-精氨酸中分離L-瓜氨酸。典型的反應(yīng)混合物(100 pL)包含50 mM HEPES,pH 7.0,8 pM 四氫生物蝶呤,1 mM CaC12,0.01 mg/mL鈣調(diào)蛋白,0.5 mM EDTA,0.450 pM [14C]-精氨酸(30000 cpm),和100-200 pM NADPH。NADPH被cNOS催化氧化為NADP+,通過Kontron 860分光光度計,在300 pL體積中340 nm下吸光度的減少監(jiān)測。除非另有說明,所有反應(yīng)在30 ℃下進行。
細胞實驗 細胞系 rMC-1細胞
濃度 1 mM
孵育時間 5天
方法 rMC-1細胞與5或25mM葡萄糖,l-NAME (1 mM)存在或不存在下培育。培養(yǎng)基每隔一天更換,進行5天。BREC細胞與5或25mM葡萄糖以及抑制劑在上述條件下培育5天。細胞死亡通過光學顯微鏡使用血細胞計數(shù)器和0.4%臺盼藍染色排除法測定。沒有被染料排除的細胞數(shù)量以每1,000個總細胞表達。每個試驗至少計數(shù)800個細胞(8個培養(yǎng)皿,每個培養(yǎng)皿細胞計數(shù)>100),并且試驗在不同的日子重復三次。
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 L-NAME(0.03-300 mg kg-1, i.v.)誘導平均全身動脈血壓劑量依賴性增加,伴隨心動過緩。L-NAME (100 mg kg-1, i.v.)顯著抑制對Ach和緩激肽的降壓反應(yīng)。L-NAME引起的血壓增加和心動過緩被L-arginine (30-100 mg kg-1, i.v.)劑量依賴性逆轉(zhuǎn)。[2]
動物實驗 Animal Models 雄性Wistar大鼠
Dosages 100 mg/kg
Administration i.v.

化學信息&溶解度

分子量 269.69 分子式

C7H15N5O4.HCl

CAS號 51298-62-5 SDF Download L-NAME HCl SDF
Smiles COC(=O)C(CCCN=C(N)N[N+](=O)[O-])N.Cl
儲存條件(自收到貨起)

體外溶解度
批次:

Water : 54 mg/mL (200.22 mM)

DMSO : Insoluble ( ;DMSO吸濕會降低化合物溶解度,請使用新開封DMSO)

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次:

現(xiàn)配現(xiàn)用,請按從左到右的順序依次添加,澄清后再加入下一溶劑

動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計算器(澄清溶液)

第一步:請輸入基本實驗信息(考慮到實驗過程中的損耗,建議多配一只動物的藥量)

mg/kg g μL

第二步:請輸入動物體內(nèi)配方組成(配方適用于不溶于水的藥物;不同批次藥物配方比例不同,請聯(lián)系Selleck為您提供正確的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結(jié)果:

工作液濃度: mg/ml;

DMSO母液配制方法: mg 藥物溶于μL DMSO溶液(母液濃度mg/mL,:如該濃度超過該批次藥物DMSO溶解度,請先聯(lián)系Selleck);

體內(nèi)配方配制方法:μL DMSO母液,加入μL PEG300,混勻澄清后加入μL Tween 80,混勻澄清后加入μL ddH2O,混勻澄清。

體內(nèi)配方配制方法:μL DMSO母液,加入μL Corn oil,混勻澄清。

注意:1. 首先保證母液是澄清的;
2.一定要按照順序依次將溶劑加入,進行下一步操作之前必須保證上一步操作得到的是澄清的溶液,可采用渦旋、超聲或水浴加熱等物理方法助溶。

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