1. GPCR/G Protein PI3K/Akt/mTOR MAPK/ERK Pathway NF-κB Metabolic Enzyme/Protease Immunology/Inflammation Apoptosis
  2. GLP Receptor Akt MEK Reactive Oxygen Species (ROS) Apoptosis MMP
  3. Lixisenatide acetate

Lixisenatide acetate  (Synonyms: 醋酸利西拉肽)

目录号: HY-P0119A 纯度: 99.65%
COA 产品使用指南 技术支持

Lixisenatide acetate 是一种胰高血糖素样肽-1 (GLP-1) 受体激动剂。Lixisenatide acetate 通过下调促炎细胞因子来抑制炎症反应,并抑制 Akt-MEK1/2 信号通路。Lixisenatide acetate 能够抑制氧化应激、线粒体功能障碍和细胞凋亡 (apoptosis)。Lixisenatide acetate 可用于炎症、代谢性疾病、神经系统疾病和心血管疾病的研究,如类风湿性关节炎、糖尿病、阿尔茨海默病和动脉粥样硬化。

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Lixisenatide acetate

Lixisenatide acetate Chemical Structure

CAS No. : 1997361-87-1

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Other Forms of Lixisenatide acetate:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Lixisenatide acetate is a glucagon-like peptide-1 (GLP-1) receptor agonist. Lixisenatide acetate inhibits the inflammatory response through down regulation of pro-inflammatory cytokines, and suppresses of the Akt-MEK1/2 signaling pathway. Lixisenatide acetate can inhibit oxidative stress, mitochondrial dysfunction and apoptosis. Lixisenatide acetate can be used for the researches of inflammation, metabolic disease, neurological disease and cardiovascular disease, such as rheumatoid arthritis, diabetes, Alzheimer's disease and atherosclerosis[1][2][3][4][5][6].

IC50 & Target[1]

GLP-1

 

MEK1

 

MEK2

 

MMP-1

 

MMP-3

 

MMP13

 

体外研究
(In Vitro)

Lixisenatide acetate (100 μM, 24 h) 抑制 Aβ25-35 (HY-P0128) 诱导的海马细胞毒性[1]
Lixisenatide acetate (100 μM, 24 h) 缓解 Aβ25-35 对海马细胞 Akt-MEK1/2 信号通路的抑制作用[1]
Lixisenatide acetate (10-20 μM, 48 h) 改善 IL-1β 诱导的氧化应激、线粒体功能障碍和成纤维样滑膜细胞凋亡[3]
Lixisenatide acetate (10-20 μM, 48 h) 减少 IL-1β 诱导 MMPs 的表达,并抑制了在成纤维样滑膜细胞中 IL-1β 的促炎通路的激活[3]
Lixisenatide acetate (10-20 μM, 6 h) 减少氧糖剥夺/再灌注诱导的人脐血管内皮细胞 ROS 生成[5]

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

Western Blot Analysis[1]

Cell Line: Fibroblast-like synoviocytes
Concentration: 10 and 20 μM
Incubation Time: 48 h
Result: Significantly reduced expression of MMP-1, MMP-3, and MMP-13 at both the mRNA and protein levels in a dose-dependent manner.
体内研究
(In Vivo)

Lixisenatide acetate (10 μg/kg,皮下注射, 一天一次持续一个月) 可减轻 Apoe−/− Irs2+/− 小鼠动脉粥样硬化负荷和全身性炎症[2]
Lixisenatide acetate (1 nmol/kg,腹腔注射, 一天一次,连续 14 天 ) 在糖尿病大鼠中对实验性早期糖尿病肾病具有肾脏保护作用[4]
Lixisenatide acetate (1-10 mg/kg,腹腔注射,每日一次,持续 10 周) 可改善 APP/PS1 小鼠的认知能力[6]

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

Animal Model: Apoe−/− Irs2+/− mice models[2]
Dosage: 10 μg/kg
Administration: Subcutaneously injection, daily for a month
Result: Exhibited smaller atheromas in the aortic arch region.
Reduced the lesion size in cross-sections of hearts.
Animal Model: Diabetic rats[4]
Dosage: 1 nmol/kg
Administration: Intraperitoneally injection, once a day for a month
Result: Showed a significant amelioration on the elevated renal parameters.
Showed significant mitigation in renal MDA and total NOx (by 50.3 and 79.9%, respectively) and 43.9% elevation in renal total antioxidant capacity.
Averted the observed increments in iNOS and COX-2 expressions in the renal tissues of the diabetic group.
Decreased the level of TGF-β protein expression.
Animal Model: APP/PS1 mice[6]
Dosage: 1 and 10 mg/kg
Administration: Intraperitoneally injection, daily for 10 weeks
Result: Improved cognitive ability.
Prevented the reduction of synapse numbers.
Reduced amyloid plaque load and chronic inflammation response (microglial activation).
Clinical Trial
分子量

5218.79

Formula

C215H347N61O65S.6C2H4O2

CAS 号
性状

固体

颜色

White to off-white

Sequence Shortening

HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPSKKKKKK-NH2

中文名称

醋酸利西拉肽

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

H2O 中的溶解度 : 50 mg/mL (9.58 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.1916 mL 0.9581 mL 1.9162 mL
5 mM 0.0383 mL 0.1916 mL 0.3832 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 (sealed storage, away from moisture)。-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)

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 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: PBS

    Solubility: 100 mg/mL (19.16 mM); 澄清溶液; 超声助溶

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

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料
参考文献

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 (sealed storage, away from moisture)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 0.1916 mL 0.9581 mL 1.9162 mL 4.7904 mL
5 mM 0.0383 mL 0.1916 mL 0.3832 mL 0.9581 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.

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产品名称:
Lixisenatide acetate
目录号:
HY-P0119A
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