1400W 2HCl
别名: N-(3-(Aminomethyl)benzyl)acetamidine 中文名称：N-[3-(氨甲基)苄基]乙脒二盐酸盐
1400W (N-(3-(Aminomethyl)benzyl)acetamidine) 是iNOS的抑制剂，与iNOS缓慢、紧密地结合，具有选择性。
1400W 2HCl Chemical Structure
CAS: 214358-33-5
客户使用Selleck的发表文献12篇
产品质控
1400W 2HCl相关产品
| 相关靶点 | nNOS eNOS iNOS | 点击展开 |
|---|---|---|
| 相关产品 | L-NAME HCl Aminoguanidine hydrochloride L-Arginine HCl (L-Arg) Falcarindiol L-NMMA acetate TPEN 2',5'-Dihydroxyacetophenone | 点击展开 |
| 相关化合物库 | 激酶抑制剂库 FDA药物库 天然产物库 已知活性药物库-I 生物活性库Ⅱ | 点击展开 |
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 |
|---|---|---|---|---|---|
| RAW264.7 | Antiinflammatory assay | 50 uM | 24 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrite production at 50 uM treated 30 mins before LPS challenge measured after 24 hrs by Griess method | 20447741 |
| RAW264.7 | Antiinflammatory assay | 0.5 to 2 uM | 2 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced COX-2 expression at 0.5 to 2 uM incubated for 2 hrs prior to LPS challenge measured after 24 hrs by Western blot analysis | 23232148 |
| RAW264.7 | Antiinflammatory assay | 2 uM | 2 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as downregulation of LPS-induced iNOS mRNA expression at 2 uM incubated for 2 hrs prior to LPS challenge measured after 9 hrs by RT-PCR analysis | 23232148 |
| RAW264.7 | Antiinflammatory assay | 0.5 to 2 uM | 2 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced iNOS expression at 0.5 to 2 uM incubated for 2 hrs prior to LPS challenge measured after 24 hrs by Western blot analysis | 23232148 |
| RAW264.7 | Function assay | 4 uM | Inhibition iNOS mRNA expression levels in LPS-induced mouse RAW264.7 cells at 4 uM by RT-PCR analysis | 27542306 | |
| RAW264.7 | Function assay | 4 uM | Inhibition iNOS protein expression levels in LPS-induced mouse RAW264.7 cells at 4 uM by Western blot analysis | 27542306 | |
| RAW264.7 | Antiinflammatory assay | 24 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay, IC50=0.2μM | 23232148 | |
| RAW264.7 | Antiinflammatory assay | 20 hrs | Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as nitrite accumulation after 20 hrs by fluorimetry, IC50=0.3μM | 11678654 | |
| RAW264.7 | Antiinflammatory assay | 24 hrs | Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrite accumulation after 24 hrs, IC50=2.9μM | 15568764 | |
| RAW264.7 | Antiinflammatory assay | 24 hrs | Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as effect on NO production pretreated 1 hr before LPS challenge measured after 24 hrs, IC50=3.1μM | 11908984 | |
| RAW 264 | Function assay | 24 hrs | Inhibition of 1ug/ml LPS-stimulated nitirc oxide accumulation in RAW 264 cells after 24 hrs, IC50=5.2μM | 17320246 | |
| N9 | Antiinflammatory assay | 24 hrs | Antiinflammatory activity against mouse N9 cells assessed as inhibition of LPS/IFN-gamma-induced nitrite accumulation after 24 hrs, IC50=6.3μM | 15568764 | |
| RAW264.7 | Cytotoxicity assay | 24 hrs | Cytotoxicity against mouse RAW264.7 cells assessed as cell viability after 24 hrs by MTS assay, IC50=47.47μM | 23232148 | |
| RAW264.7 | Function assay | Inhibition of LPS-induced nitric oxide generation in mouse RAW264.7 cells pretreated 1 hr before LPS challenge by Griess method, IC50=1.5μM | 19278854 | ||
| N9 | Function assay | Inhibitory effect of compound on the accumulation of NO2 in the culture media of N9 cells in response to LPS/IFN-gamma, IC50=2.2μM | 15013012 | ||
| RAW264.7 | Antiinflammatory assay | Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of nitric oxide production pretreated 1 hr before LPS challenge, IC50=2.3μM | 12662101 | ||
| RAW264.7 | Function assay | Inhibition of LPS-induced nitric oxide accumulation in mouse RAW264.7 cells, IC50=2.7μM | 19699097 | ||
| N9 | Antiinflammatory assay | Antiinflammatory activity in LPS/IFN-gamma-stimulated mouse N9 cells assessed as inhibition of nitric oxide production pretreated 1 hr before LPS/IFNgamma challenge, IC50=3.6μM | 12662101 | ||
| RAW264.7 | Function assay | Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells, IC50=3.78μM | 17988874 | ||
| RAW264.7 | Function assay | Inhibitory effect of compound on the accumulation of NO2 in the culture media of RAW 264.7 cells in response to LPS, IC50=6.1μM | 15013012 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | 1400W (N-(3-(Aminomethyl)benzyl)acetamidine) 是iNOS的抑制剂，与iNOS缓慢、紧密地结合，具有选择性。 | ||||||
|---|---|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 1400W是一种不可逆的抑制剂或是一种具有积极缓慢的可逆性的抑制剂，抑制iNOS。1400对于人源iNOS的抑制作用是时间依赖性的。1400W与L-arginine属于竞争关系，不是iNOS的底物[1]。 | |||
|---|---|---|---|---|
| 细胞实验 | 细胞系 | RAW264.7细胞 | ||
| 浓度 | 100 μM | |||
| 孵育时间 | 16 h | |||
| 方法 | 用LPS/IFNγ和iNOS的抑制剂1400W（100 μM）处理RAW264.7，处理16小时。GAPDH-P300的结合被1400W抑制。获取细胞裂解液，用anti-p300的抗体进行免疫沉淀，免疫沉淀物用于WB分析。 | |||
| 体内研究(In Vivo) | ||
| 体内研究活性 | 1400W在大鼠中选择性地抑制微脉管系统损伤。在大鼠内毒素诱导的血管损伤模型中，1400W对iNOS的抑制作用比eNOS有效50倍以上。除此之外，1400W还在结肠、肝脏、肾脏和心脏处浓度依赖性地减少LPS诱导的、与iNOS诱导相关的血管渗漏.对于除去肾脏的其他器官，其保护作用几近100%，而在肾脏中式54%[1]。1400W在肾脏缺血再灌注的大鼠模型中，对肾脏的氧化和硝化压力具有改善作用[2]。在小鼠中，处理以1400W可以减少实体瘤的生长速率[4]。 | |
|---|---|---|
| 动物实验 | Animal Models | 大鼠 |
| Dosages | 0.1-10 mg/kg | |
| Administration | 皮下注射 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00845169 | Completed | Endothelial Dysfunction |
University of Edinburgh|NHS Lothian|Umeå University |
April 2012 | Not Applicable |
化学信息&溶解度
| 分子量 | 250.17 | 分子式 | C10H15N3.2HCl |
| CAS号 | 214358-33-5 | SDF | Download 1400W 2HCl SDF |
| Smiles | CC(=NCC1=CC=CC(=C1)CN)N.Cl.Cl | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 35 mg/mL ( (139.9 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : 35 mg/mL Ethanol : 35 mg/mL |
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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