1. GPCR/G Protein Autophagy Neuronal Signaling MAPK/ERK Pathway Protein Tyrosine Kinase/RTK Apoptosis
  2. Insulin Receptor Autophagy p38 MAPK GLP Receptor α-synuclein Bcl-2 Family Apoptosis
  3. Semaglutide acetate

Semaglutide acetate 是一种长效、选择性、竞争型、口服有效的 GLP-1R 激动剂,能透过血脑屏障。Semaglutide acetate 激活 GLP-1R 后促进胰岛素分泌、抑制胃排空和食欲,同时通过增强自噬、抑制氧化应激和凋亡 (apoptosis)。Semaglutide acetate 还调节线粒体功能及脂质代谢 (如减少肝内从头脂肪生成) 。Semaglutide acetate 具有降血糖、减重、神经保护 (如改善帕金森病模型中的运动功能、减少 α-突触核蛋白 (α-synuclein) 聚集) 及改善肝脂肪变性等活性。Semaglutide acetate 可用于 2 型糖尿病、肥胖症、帕金森病、代谢相关脂肪性肝病 (MASLD) 等神经退行性疾病和肝脏疾病,以及癌症的研究。

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Semaglutide acetate Chemical Structure

Semaglutide acetate Chemical Structure

CAS No. : 1997361-85-9

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Other Forms of Semaglutide acetate:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Semaglutide acetate is a long-acting, selective, competitive, orally active GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide acetate promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances autophagy, inhibits oxidative stress and apoptosis. Semaglutide acetate also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide acetate has activities such as lowering blood sugar, reducing weight, neuroprotection (such as improving motor function in Parkinson's disease models, reducing α-synuclein aggregation) and improving hepatic steatosis. Semaglutide acetate can be used for the study of neurodegenerative diseases and liver diseases such as type 2 diabetes, obesity, Parkinson's disease, metabolic associated fatty liver disease (MASLD), and cancer[1][2][3][4][5].

体外研究
(In Vitro)

1. 抗 Aβ25-35 损伤实验:
Semaglutide acetate (1-100 nM;24 h) 显著提高 SH-SY5Y 细胞的存活率,增加 LC3II、Atg7、Beclin-1 和 P62 等自噬相关蛋白表达,抑制 Bax 并上调 Bcl-2,通过增强自噬、抑制凋亡并保护神经细胞[1][2]
2. 口腔鳞状细胞癌 (OSCC) 细胞实验:
Semaglutide acetate (5-40 μM;48 h) 剂量依赖性抑制 Cal27 和 HSC4 细胞的增殖、迁移及侵袭,上调 E-cadherin 并下调 Vimentin,激活 P38 MAPK 信号通路 (p-P38 表达增加),诱导细胞凋亡[3]

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

Cell Viability Assay[1][2]

Cell Line: SH-SY5Y human neuroblastoma cells
Concentration: 0, 1, 10, 100 nM
Incubation Time: 24 h
Result: Cell Viability: Significantly increased cell survival rate in a dose-dependent manner, reversing Aβ25-35-induced cytotoxicity.
WB (Western Blot): Upregulated autophagy markers (LC3II, Atg7, Beclin-1, P62) and anti-apoptotic protein Bcl-2, while downregulating pro-apoptotic protein Bax.
体内研究
(In Vivo)

口腔鳞状细胞癌 (OSCC) 移植瘤模型
Semaglutide (3 μmol/kg;皮下注射;每周 3 次;3 周) acetate 显著抑制裸鼠口腔鳞状细胞癌 (OSCC) 移植瘤模型的肿瘤体积增长,下调增殖标志物 Ki67 和 PCNA,上调促凋亡蛋白 Bax 并下调抗凋亡蛋白 Bcl-xL,通过激活 P38 MAPK 通路诱导肿瘤细胞凋亡[3]
慢性 MPTP 诱导的帕金森病模型
Semaglutide (25 nmol/kg;腹腔注射;每 2 天 1 次;30 天) acetate 改善小鼠慢性 MPTP 诱导的帕金森病模型及其运动功能障碍,增加黑质酪氨酸 (TH) 阳性神经元数量,减少 α-突触核蛋白聚集及胶质细胞活化,降低氧化应激标志物 4-HNE 水平[4]
代谢功能障碍相关脂肪性肝病 (MASLD) 模型
Semaglutide (25 μg/kg/周+100 μg/kg/周;皮下注射;每周 1 次;11 周) acetate 在小鼠代谢功能障碍相关脂肪性肝病 (MASLD) 模型中,降低小鼠体重、血糖及血清肝酶 (ALT、AST、AP),减少肝内甘油三酯沉积,改善肝脂肪变性及肝细胞气球样变,下调从头脂肪生成标志物 Acaca 和 Scd1[5]

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

Animal Model: BALB/c nude mice (male, 4-6 weeks old) with oral squamous cell carcinoma (OSCC) xenograft model[3]
Dosage: 3 μmol/kg Semaglutide
Administration: Subcutaneous injection, 3 times weekly, for 3 weeks
Result: Significantly reduced tumor volume and weight compared to the control group.
Decreased expression of proliferation markers (Ki67, PCNA) and mesenchymal marker Vimentin, while increasing epithelial marker E-cadherin.
Clinical Trial
CAS 号
性状

固体

颜色

White to off-white

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: 

DMSO 中的溶解度 : ≥ 100 mg/mL

* "≥" means soluble, but saturation unknown.

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纯度 & 产品资料

纯度: 99.92%

参考文献
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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Semaglutide acetate
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HY-114118B
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