L-NAME HCl
别名: NG-Nitroarginine methyl ester, N-Nitro-L-arginine methylester
L-NAME HCl (NG-Nitroarginine methyl ester, N-Nitro-L-arginine methylester)是一种无选择性的一氧化氮合成酶抑制剂，对nNOS (牛源), eNOS (人源)和iNOS (鼠源)的Ki值分别为15nM, 39 nM和4.4 μM。
L-NAME HCl Chemical Structure
CAS: 51298-62-5
客户使用Selleck的L-NAME HCl发表文献37篇
产品质控
NOS抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | L-NAME HCl (NG-Nitroarginine methyl ester, N-Nitro-L-arginine methylester)是一种无选择性的一氧化氮合成酶抑制剂，对nNOS (牛源), eNOS (人源)和iNOS (鼠源)的Ki值分别为15nM, 39 nM和4.4 μM。 | ||||
|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | NG-硝基-L-精氨酸甲酯(L-NAME; 0.1-100 mM)浓度依赖性抑制猪主动脉中Ca2(+)-依赖性内皮NO合酶。L-NAME引起主动脉环中内皮细胞依赖性收缩，以及乙酰胆碱(ACh)诱导的血管内皮依赖性舒张反应的抑制。[2]在另一项研究中，rMC-1细胞或BREC在25 mM葡萄糖中的活性显著比在5 mM葡萄糖中低，这种细胞死亡在两种细胞类型中被l-NAME抑制。[3] | |||
|---|---|---|---|---|
| 激酶实验 | 酶测定 | |||
| L-精氨酸的氧化通过[3H]-或[14C]-精氨酸转化为L-瓜氨酸监测，通过Dowex 50x8-200 (Na)色谱分析从L-精氨酸中分离L-瓜氨酸。典型的反应混合物(100 pL)包含50 mM HEPES，pH 7.0，8 pM 四氢生物蝶呤，1 mM CaC12，0.01 mg/mL钙调蛋白，0.5 mM EDTA，0.450 pM [14C]-精氨酸(30000 cpm)，和100-200 pM NADPH。NADPH被cNOS催化氧化为NADP+，通过Kontron 860分光光度计，在300 pL体积中340 nm下吸光度的减少监测。除非另有说明，所有反应在30 ℃下进行。 | ||||
| 细胞实验 | 细胞系 | rMC-1细胞 | ||
| 浓度 | 1 mM | |||
| 孵育时间 | 5天 | |||
| 方法 | rMC-1细胞与5或25mM葡萄糖，l-NAME (1 mM)存在或不存在下培育。培养基每隔一天更换，进行5天。BREC细胞与5或25mM葡萄糖以及抑制剂在上述条件下培育5天。细胞死亡通过光学显微镜使用血细胞计数器和0.4%台盼蓝染色排除法测定。没有被染料排除的细胞数量以每1,000个总细胞表达。每个试验至少计数800个细胞(8个培养皿，每个培养皿细胞计数>100)，并且试验在不同的日子重复三次。 | |||
| 体内研究(In Vivo) | ||
| 体内研究活性 | L-NAME(0.03-300 mg kg-1, i.v.)诱导平均全身动脉血压剂量依赖性增加，伴随心动过缓。L-NAME (100 mg kg-1, i.v.)显著抑制对Ach和缓激肽的降压反应。L-NAME引起的血压增加和心动过缓被L-arginine (30-100 mg kg-1, i.v.)剂量依赖性逆转。[2] | |
|---|---|---|
| 动物实验 | Animal Models | 雄性Wistar大鼠 |
| Dosages | 100 mg/kg | |
| Administration | i.v. | |
化学信息&溶解度
| 分子量 | 269.69 | 分子式 | C7H15N5O4.HCl |
| CAS号 | 51298-62-5 | SDF | Download L-NAME HCl SDF |
| Smiles | COC(=O)C(CCCN=C(N)N[N+](=O)[O-])N.Cl | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
Water : 54 mg/mL DMSO : Insoluble ( DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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