中文名称: | 拉扎贝胺 | ||||
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英文名称: | Lazabemide | ||||
别名: | 拉扎贝胺 Cardaptive; MK-0524;MK0524; Laropiprant;Cyclopent(b)indole-3-acetic acid, 4-((4-chlorophenyl)methyl)-7-fluoro-1,2,3,4-tetrahydro-5-(methylsulfonyl)-, (3R)- | ||||
CAS No: | 103878-84-8 | 分子式: | C21H19ClFNO4S | 分子量: | 435.90 |
CAS No: | 103878-84-8 | ||||
分子式: | C21H19ClFNO4S | ||||
分子量: | 435.90 |
基本信息
产品编号: |
L10234 |
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产品名称: |
Lazabemide |
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CAS: |
103878-84-8 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
两年 |
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分子量 |
435.90 |
-20℃ |
一个月 |
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化学名: |
N-(2-Aminoethyl)-5-chloro-2-pyridinecarboxamide;N-(2-Aminoethyl)-5-chloro-2-pyridinecarboxamide |
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Solubility (25°C): |
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体外:
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DMSO |
5mg/mL (25.05mM; Need ultrasonic) |
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Ethanol |
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Water |
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体内(现配现用): |
1.请依序添加每种溶剂:10% DMSO→40% PEG300→5% Tween-80→45% saline,Solubility: ≥ 0.5mg/mL(2.50mM); Clear solution |
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此⽅案可获得 ≥ 0.5mg/mL (2.50mM,饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例,取 100μL 5.0mg/mL 的澄清 DMSO 储备液加到 400μL PEG300 中,混合均匀;向上述体系中加⼊ 50μL Tween-80,混合均匀;然后继续加⼊ 450μL ⽣理盐⽔定容⾄ 1mL。 |
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2.请依序添加每种溶剂:10% DMSO→90% (20% SBE-β-CD in saline) Solubility: ≥ 0.5mg/mL (2.50mM); Clear solution |
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此⽅案可获得 ≥ 0.5 mg/mL (2.50mM,饱和度未知) 的澄清溶液。以 1mL ⼯作液为例,取 100μL 5.0 mg/mL 的澄清 DMSO 储备液加到 900μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中,混合均匀 。 |
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3.请依序添加每种溶剂:10% DMSO→90% corn oil Solubility:: ≥ 0.5mg/mL (2.50mM); Clear solution |
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此⽅案可获得 ≥ 0.5mg/mL (2.50mM,饱和度未知) 的澄清溶液,此⽅案不适⽤于实验周期在半个⽉以上的实验。 以 1mL ⼯作液为例,取 100μL 5.0mg/mL 的澄清 DMSO 储备液加到 900μL ⽟⽶油中,混合均匀。 |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
5.0090mL |
25.0451mL |
50.0902mL |
5mM |
1.0018mL |
5.0090mL |
10.0180mL |
10mM |
0.5009mL |
2.5045mL |
5.0090mL |
生物活性
产品描述 |
一种单胺氧化酶B(MAO-B))的选择性的可逆抑制剂,IC50=0.03μM。 |
靶点 |
IC50: 30nM (MAO-B) |
体外研究 |
The in vitro binding characteristics of both radiolabeled inhibitors revealed them to be selective, high-affinity ligands for the respective enzymes. KD and Bmax values for 3H-Ro 19-6327 in rat cerebral cortex are 18.4 nM and 3.45 pmol/mg protein, respectively. The IC50 values for lazabemide are: 86μM for NA uptake; 123μM for 5HT uptake; > 500μM for DA uptake, respectively. Lazabemide (5μM) inhibits human MAO-B and MAO-A with IC50 of 6.9nM and >10nM, respectively. And it inhibits rat MAO-B and MAO-A with IC50of 37nM and >10μM, respectively ina enzymatic assay. Lazabemide differs from L-deprenyl in their ability to induce release of endogenous monoamines from synaptosomes. Thus, Lazabemide (500μM) induces a greater 5 HT release than does L-deprenyl, but is less effective than L-deprenyl in releasing DA. On the contrary, lazabemide was almost completely inactive on either 5-HT and DA release. Lazabemide (250nM) results in a clear inhibition of DOPAC formation, while does not increase the accumulation of newlyformed DA in those tubular epithelial cells loaded with 50microM L-DOPA. |
体内研究 |
Lazabemide (3mg/kg) attenuates ichemia reperfusion-induced hydroxyl radical generation and pretreatment with Lazabemide showed decreased DOPAC levels in comparison with those of their respective vehicle-treated control groups. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )