Rasagiline (Synonyms: 雷沙吉兰; (R)-AGN1135; TVP1012)

目录号: HY-14605A 纯度: 99.88%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Rasagiline (R-AGN1135) 是一种高效的不可逆的选择性线粒体单胺氧化酶 (MAO) 抑制剂，抑制大鼠脑 MAO B 和 MAO A 的 IC₅₀ 分别为 4.43 nM 和 412 nM。Rasagiline 是一种点击化学试剂。它含有 Alkyne 基团，可以和含有 Azide 基团的分子发生铜催化的叠氮-炔环加成反应 (CuAAc)。

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Rasagiline Chemical Structure

CAS No. : 136236-51-6

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1100	In-stock
50 mg	￥1000	In-stock
100 mg	￥1246	In-stock
200 mg		询价
500 mg		询价

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Other Forms of Rasagiline:

MCE 顾客使用本产品发表的 6 篇科研文献

: Rasagiline purchased from MCE. Usage Cited in: Oncotarget. 2018 Jan 30;9(15):12137-12153. [Abstract]; Retinal protection of Rasagiline combined with Idebenone against retinal ischemia-reperfusion (RIR) injury. Western blot analysis for the expression level of brain-derived neurotrophic factor (BDNF) in the whole IR-injured retinas.

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MAO-A MAO-B

生物活性
纯度 & 产品资料
参考文献

生物活性

Rasagiline (R-AGN1135) is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC₅₀s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively^[1]. Rasagiline is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC₅₀ & Target^[1]

rMAO-B

4.43 nM (IC₅₀)

rMAO-A

412 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
BTI-TN-5B1-4	IC₅₀	0.069 μM Compound: Rasagiline	Inhibition of human recombinant microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate assessed as production of H2O2 incubated for 15 mins followed by substrate addition measured over 15 mins by fluorimetric a Inhibition of human recombinant microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate assessed as production of H2O2 incubated for 15 mins followed by substrate addition measured over 15 mins by fluorimetric a	[PMID: 23474901]
BTI-TN-5B1-4	IC₅₀	13 nM Compound: Rasagiline	Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as decrease in H2O2 production using p-tyramine as substrate incubated for 20 mins by horse-radish peroxidase/amplex red-based fluorescence method Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as decrease in H2O2 production using p-tyramine as substrate incubated for 20 mins by horse-radish peroxidase/amplex red-based fluorescence method	[PMID: 31265934]
BTI-TN-5B1-4	IC₅₀	13 nM Compound: Rasagiline	Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by resorufin-based fluorescence assay Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by resorufin-based fluorescence assay	[PMID: 30522087]
BTI-TN-5B1-4	IC₅₀	147.3 μM Compound: Rasagiline	Inhibition of human microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as reduction in 4-hydroxyquinoline formation using kynuramine as substrate preincubated with substrate for 10 mins followed by enzyme addition by spectropho Inhibition of human microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as reduction in 4-hydroxyquinoline formation using kynuramine as substrate preincubated with substrate for 10 mins followed by enzyme addition by spectropho	[PMID: 31711793]
BTI-TN-5B1-4	IC₅₀	16.44 μM Compound: Rasagiline	Inhibition of human recombinant microsomal MAO-A expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate assessed as production of H2O2 incubated for 15 mins followed by substrate addition measured over 15 mins by fluorimetric a Inhibition of human recombinant microsomal MAO-A expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate assessed as production of H2O2 incubated for 15 mins followed by substrate addition measured over 15 mins by fluorimetric a	[PMID: 23474901]
BTI-TN-5B1-4	IC₅₀	3.65 μM Compound: Rasagiline	Inhibition of human microsomal MAO-A expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as reduction in 4-hydroxyquinoline formation using kynuramine as substrate preincubated with substrate for 10 mins followed by enzyme addition by spectropho Inhibition of human microsomal MAO-A expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as reduction in 4-hydroxyquinoline formation using kynuramine as substrate preincubated with substrate for 10 mins followed by enzyme addition by spectropho	[PMID: 31711793]
BTI-TN-5B1-4	IC₅₀	49.66 nM Compound: Rasagline	Inhibition of human microsomal MAO-B expressed in recombinant baculovirus infected insect BTI-TN-5B1-4 cells assessed as reduction in H2O2 production using p-tyramine as substrate after 15 mins by fluorescence assay Inhibition of human microsomal MAO-B expressed in recombinant baculovirus infected insect BTI-TN-5B1-4 cells assessed as reduction in H2O2 production using p-tyramine as substrate after 15 mins by fluorescence assay	[PMID: 27244485]
BTI-TN-5B1-4	IC₅₀	52974 nM Compound: Rasagline	Inhibition of human microsomal MAO-A expressed in recombinant baculovirus infected insect BTI-TN-5B1-4 cells assessed as reduction in H2O2 production using p-tyramine as substrate after 15 mins by fluorescence assay Inhibition of human microsomal MAO-A expressed in recombinant baculovirus infected insect BTI-TN-5B1-4 cells assessed as reduction in H2O2 production using p-tyramine as substrate after 15 mins by fluorescence assay	[PMID: 27244485]
BTI-TN-5B1-4	IC₅₀	680 nM Compound: Rasagiline	Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as decrease in H2O2 production using p-tyramine as substrate incubated for 20 mins by horse-radish peroxidase/amplex red-based fluorescence method Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as decrease in H2O2 production using p-tyramine as substrate incubated for 20 mins by horse-radish peroxidase/amplex red-based fluorescence method	[PMID: 31265934]
BTI-TN-5B1-4	IC₅₀	680 nM Compound: Rasagiline	Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by resorufin-based fluorescence assay Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by resorufin-based fluorescence assay	[PMID: 30522087]
SH-SY5Y	IC₅₀	2700 μM Compound: Rasagiline	Cytotoxicity against human SH-SY5Y cells measured after 24 hrs by MTT assay Cytotoxicity against human SH-SY5Y cells measured after 24 hrs by MTT assay	[PMID: 33360800]
SIM-A9	IC₅₀	2900 μM Compound: Rasagiline	Cytotoxicity against mouse SIM-A9 cells measured after 24 hrs by MTT assay Cytotoxicity against mouse SIM-A9 cells measured after 24 hrs by MTT assay	[PMID: 33360800]

体外研究
(In Vitro)

Rasagiline (0.25 nM；96 小时) 在 Dexamethasone (10 μM) 处理后显著增加 SH-SY5Y 和 1242-MG 的增殖率^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[2]

Cell Line:	Neuroblastoma SH-SY5Y, and glioblastoma 1242-MG
Concentration:	0.25 nM
Incubation Time:	96 hours
Result:	Caused ~60% increase in the cell proliferation rate for SH-SY5Y cells treated with Dexamethasone. Caused ~35% increase in cell proliferation rate for 1242-MG cells treated with Dexamethasone.

体内研究
(In Vivo)

Rasagiline 在多系统萎缩的转基因模型中具有神经保护作用。运动行为测试显示 2.5 mg/kg 雷沙吉兰疗法可改善运动缺陷^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	(PLP)-α-synuclein transgenic mice over 6 months of age^[3]
Dosage:	Low-(0.8 mg/kg b.w.) and high dose (2.5 mg/kg b. w.)
Administration:	Administered subcutaneously every 24 h for a total period of 4 weeks (from day 1 till day 28 of the experiment).
Result:	Low dose treatment did not show protective efficacy in striatum with number of neurons similar to placebo treated MSA mice. High dose was associated with about 15% rescue of DARPP-32 immunoreactive striatal neurons. Low dose treatment had no effect on nigral neuronal loss, but high dose completely protected nigral neurons with numbers comparable to healthy controls.

Clinical Trial

分子量

171.24

Formula

C₁₂H₁₃N

CAS 号

136236-51-6

性状

<38°C 固体,>41°C 液体

颜色

Light yellow to brown

中文名称

雷沙吉兰

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : 100 mg/mL (583.97 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H₂O 中的溶解度 : ≥ 5.88 mg/mL (34.34 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	5.8397 mL	29.1983 mL	58.3965 mL
5 mM	1.1679 mL	5.8397 mL	11.6793 mL
10 mM	0.5840 mL	2.9198 mL	5.8397 mL

查看完整储备液配制表

* 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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (14.60 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (14.60 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (14.60 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.88%

选择批次：

Data Sheet (641 KB) SDS (393 KB)

COA (287 KB) HNMR (217 KB) LCMS (257 KB)

产品使用指南 (1538 KB)

参考文献

[1]. M B Youdim, et al. Rasagiline [N-propargyl-1R(+)-aminoindan], a selective and potent inhibitor of mitochondrial monoamine oxidase B. Br J Pharmacol. 2001 Jan;132(2):500-6. [Content Brief]

[2]. Shawna Tazik, et al. Comparative neuroprotective effects of Rasagiline and aminoindan with selegiline on dexamethasone-induced brain cell apoptosis. Neurotox Res. 2009 Apr;15(3):284-90. [Content Brief]

[3]. Nadia Stefanova, et al. Rasagiline is neuroprotective in a transgenic model of multiple system atrophy. Exp Neurol. 2008 Apr;210(2):421-7. [Content Brief]

Rasagiline 相关分类

Neurological Disease

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	5.8397 mL	29.1983 mL	58.3965 mL	145.9914 mL
	5 mM	1.1679 mL	5.8397 mL	11.6793 mL	29.1983 mL
	10 mM	0.5840 mL	2.9198 mL	5.8397 mL	14.5991 mL
	15 mM	0.3893 mL	1.9466 mL	3.8931 mL	9.7328 mL
	20 mM	0.2920 mL	1.4599 mL	2.9198 mL	7.2996 mL
	25 mM	0.2336 mL	1.1679 mL	2.3359 mL	5.8397 mL
	30 mM	0.1947 mL	0.9733 mL	1.9466 mL	4.8664 mL
DMSO	40 mM	0.1460 mL	0.7300 mL	1.4599 mL	3.6498 mL
	50 mM	0.1168 mL	0.5840 mL	1.1679 mL	2.9198 mL
	60 mM	0.0973 mL	0.4866 mL	0.9733 mL	2.4332 mL
	80 mM	0.0730 mL	0.3650 mL	0.7300 mL	1.8249 mL
	100 mM	0.0584 mL	0.2920 mL	0.5840 mL	1.4599 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rasagiline136236-51-6(R)-AGN1135 TVP1012雷沙吉兰TVP1012TVP 1012TVP-1012Monoamine OxidaseMAOInhibitorinhibitorinhibit

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Rasagiline (Synonyms: 雷沙吉兰; (R)-AGN1135; TVP1012)

Customer Review

Other Forms of Rasagiline:

MCE 顾客使用本产品发表的 6 篇科研文献

Rasagiline 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Monoamine Oxidase 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

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稀释计算器

Rasagiline 相关分类

完整储备液配制表

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Rasagiline (Synonyms: 雷沙吉兰; (R)-AGN1135; TVP1012)

Customer Review

Other Forms of Rasagiline:

Rasagiline 相关抗体

MCE 顾客使用本产品发表的 6 篇科研文献

Rasagiline 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Monoamine Oxidase 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

Rasagiline 相关抗体:

摩尔计算器

稀释计算器

Rasagiline 相关分类

完整储备液配制表

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