拉扎贝胺 - CAS:103878-84-8 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	拉扎贝胺
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

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L10234 拉扎贝胺 ≥98% (psaitong)

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包装规格：

10mg 50mg 100mg in glass bottle

溶解性：

溶于DMSO(超声)

产品描述：

基本信息

产品编号：	L10234
产品名称：	Lazabemide
CAS:	103878-84-8	储存条件	粉末	-20℃	四年

分子式：	C21H19ClFNO4S		溶于液体	-80℃	两年
分子量	435.90			-20℃	一个月
化学名：	N-(2-Aminoethyl)-5-chloro-2-pyridinecarboxamide;N-(2-Aminoethyl)-5-chloro-2-pyridinecarboxamide
Solubility (25°C)：
体外:	DMSO	5mg/mL (25.05mM; Need ultrasonic)
	Ethanol
	Water
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
	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。
	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
	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。
	3.请依序添加每种溶剂：10% DMSO→90% corn oil Solubility:: ≥ 0.5mg/mL (2.50mM); Clear solution
	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。
＜1mg/ml表示微溶或不溶。
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。
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.