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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 可用于誘導高血壓動物模型。
L-NAME HCl Chemical Structure
CAS: 51298-62-5
產(chǎn)品質(zhì)控
批次：
純度：
99.94%
99.94
L-NAME HCl相關(guān)產(chǎn)品
| 相關(guān)靶點 | nNOS eNOS iNOS | 點擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | 1400W 2HCl 2',5'-Dihydroxyacetophenone TPEN L-NMMA acetate | 點擊展開 |
| 相關(guān)化合物庫 | 激酶抑制劑庫 FDA藥物庫 天然產(chǎn)物庫 已知活性藥物庫-I 高選擇性抑制劑庫 | 點擊展開 |
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(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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
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。L-NAME HCl 可用于誘導高血壓動物模型。 | ||||
|---|---|---|---|---|---|
| 靶點 |
|
| 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。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 |
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)溶解配方 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
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
只
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，注：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：取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：取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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