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/ Glucagon Receptor / Semaglutide/司美格鲁肽

Semaglutide/司美格鲁肽 {[allProObj[0].p_purity_real_show]}

货号：A753934 同义名： 索马鲁肽;索玛鲁肽

Semaglutide 是一种长效人类 GLP-1 类似物，作为 GLP-1 受体激动剂，常用于 2 型糖尿病的研究。

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Semaglutide/司美格鲁肽 化学结构 CAS号：910463-68-2
Semaglutide/司美格鲁肽 化学结构
CAS号：910463-68-2
Semaglutide/司美格鲁肽 3D分子结构
CAS号：910463-68-2
Semaglutide/司美格鲁肽 化学结构 CAS号：910463-68-2
Semaglutide/司美格鲁肽 3D分子结构 CAS号：910463-68-2
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Semaglutide/司美格鲁肽 纯度/质量文件 产品仅供科研

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全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
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• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
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Semaglutide/司美格鲁肽 生物活性

描述 Semaglutide is a GLP-1 receptor agonist with affinity value of 0.38nM to GLP-1R. It is used as a once weekly GLP-1 analog to treat type 2 diabetes and obesity. Semaglutide exhibited effect on lowering blood glucose with an EC50 of <2 nmol/kg up to 48 h in db/db mice[1]. Intraperitoneal injection with 25 nmol/kg semaglutide once every two days for 30 days exhibited neuroprotective effects on the chronic MPTP mouse model of Parkinson’s disease. It improved MPTP-induced motor impairments, rescued the decrease of tyrosine hydroxylase (TH) levels, reduced the accumulation of α-syn, alleviated the chronic inflammation response in the brain, reduced lipid peroxidation, and inhibited the mitochondrial mitophagy signaling pathway, and furthermore increased expression of the key growth factor GDNF that protects dopaminergic neurons in the substantia nigra (SN) and striatum[2]. Administration of semaglutide significantly attenuated plaque lesion development in ApoE-/- mice and LDLr-/- mice. Also it significantly reversed expression of genes in pathways relevant to the pathogenesis of atherosclerosis, through an anti-inflammatory mechanism, in aortic tissue of animals exposure to a Western diet[3].
作用机制 Semaglutide is a GLP-1 analogue with two amino acid substitutions compared to human GLP-1 (Aib8, Arg34) and is derivatized at lysine 26. It forms a complex with the GLP-1 receptor extracellular domain.[1]

Semaglutide/司美格鲁肽 细胞实验

Cell Line
Concentration Treated Time Description References
Human Aortic Endothelial Cells (HAEC) 1 nM 20 hours To study the effect of Semaglutide on angiogenesis, results showed that Semaglutide combined with FABP4 significantly increased angiogenesis Cardiovasc Diabetol. 2024 Jan 3;23(1):1
BV2 cells 900 nM 20 hours To evaluate the effect of Semaglutide on BV2 cell proliferation, results showed that 900 nM Semaglutide minimally impacted cell viability and exhibited no cytotoxicity. Int J Mol Med. 2021 Dec;48(6):219
Neutrophil-like dHL-60 cells 1 nM 90 minutes To study the effect of Semaglutide on CD11b expression in neutrophils, results showed that Semaglutide modulated FABP4-induced upregulation of CD11b Cardiovasc Diabetol. 2024 Jan 3;23(1):1

Semaglutide/司美格鲁肽 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice and rats Alcohol dependence model Subcutaneous injection 0.001, 0.003, 0.01, 0.03, 0.1 mg/kg (mice); 0.001, 0.01, 0.1 mg/kg (rats) Two doses per week Semaglutide dose-dependently reduced binge-like alcohol drinking in mice and rats, and reduced alcohol self-administration in alcohol-dependent rats. Additionally, Semaglutide increased sIPSC frequency in CeA and ILC neurons from alcohol-naive rats, suggesting enhanced GABA release, but had no overall effect on GABA transmission in alcohol-dependent rats. JCI Insight. 2023 Jun 22;8(12):e170671
Rats and mice Intermittent access model Subcutaneous injection 0.026 mg/kg and 0.052 mg/kg Once a week for three weeks Semaglutide significantly reduced alcohol intake and prevented relapse-like drinking in male and female rats. Moreover, fluorescently labelled semaglutide was detected in NAc of alcohol-drinking male and female rats. Further, semaglutide attenuated the ability of alcohol to cause hyperlocomotion and to elevate dopamine in NAc in male mice. EBioMedicine. 2023 Jul;93:104642
C57BL/6J mice Polycystic ovary syndrome (PCOS) model Subcutaneous injection 0.42 mg/kg/w and 0.84 mg/kg/w Once a week for 4 weeks Semaglutide alleviates ovarian inflammation via the AMPK/SIRT1/NF-κB signaling pathway in PCOS mice. Drug Des Devel Ther. 2024 Sep 4;18:3925-3938
Wistar rats Streptozotocin-induced diabetic neuropathy model Oral 1.44 mg/kg or 2.88 mg/kg Once daily for 4 weeks Teneligliptin reduced spinal astrocyte activation and neuropathic pain caused by partial sciatic nerve transection. Additionally, it improved the analgesic effects of morphine and reduced analgesic tolerance. Cells. 2024 Nov 8;13(22):1857
C57BL/6J mice PTZ kindling model Intraperitoneal injection 10 nM/kg and 25 nM/kg Administered every other day for 37 days To evaluate the effects of Semaglutide on seizure severity, cognitive dysfunction, and hippocampal neuronal apoptosis in PTZ-kindled mice. Results showed that Semaglutide reduced seizure severity, ameliorated cognitive dysfunction, and decreased hippocampal neuronal apoptosis. Int J Mol Med. 2021 Dec;48(6):219
Human Adults with overweight or obesity Subcutaneous injection 2.4 mg Once weekly for 68 weeks To evaluate the effects of semaglutide on cardiometabolic risk factors in adults with overweight or obesity. Results showed that semaglutide significantly improved waist circumference, systolic blood pressure, diastolic blood pressure, fasting plasma glucose, fasting serum insulin, lipids, and HOMA-IR compared to placebo. Diabetes Obes Metab. 2023 Feb;25(2):468-478
C57BL/6J mice HFD-induced NAFLD model Intraperitoneal injection 30 mmol/kg Once daily for 12 weeks To evaluate the effects of Semaglutide on body weight, liver weight, blood glucose, liver injury markers, pro-inflammatory factors, and oxidative stress marker levels in HFD-induced NAFLD model mice. Results showed that Semaglutide significantly reduced body weight, liver weight, blood glucose, TG, TCHO, LDL, and pro-inflammatory factors, while increasing SOD levels. Additionally, Semaglutide significantly improved liver histopathological changes such as hepatocyte steatosis, balloon degeneration, and lymphoid foci, and reduced lipid droplet deposition. Front Endocrinol (Lausanne). 2022 Dec 9;13:1046130
Male C57BL/6J mice GAN diet-induced obese and biopsy-confirmed NASH-HCC mouse model Subcutaneous injection 30 nmol/kg Once daily for 14 weeks To evaluate the therapeutic effects of Semaglutide on NASH and tumor burden. Results showed that Semaglutide significantly improved histological features of NASH and reduced tumor burden. Sci Rep. 2023 Dec 27;13(1):23056
Male mice Pressure overload-induced heart failure model (TAC surgery) Intraperitoneal injection 4.0, 12.0 or 60.0 μg/kg/day Once daily for eight weeks To investigate the effect of Semaglutide on TAC-induced heart failure, results showed that Semaglutide improved cardiac function, reduced hypertrophy and fibrosis, and preserved mitochondrial structure and function. Nat Commun. 2024 Jun 4;15(1):4757

Semaglutide/司美格鲁肽 动物研究

Dose Rat: 0.15 mg/kg, 0.48 mg/kg[4] (s.c.)
Administration s.c.
Pharmacokinetics
Animal Mice[5] Rats[5] Monkeys[5]
Dose 1 mg/kg 1 mg/kg 1 mg/kg
Administration s.c. s.c. s.c.
Cavg 927 nmol/l 2080 nmol/l
Cmean 522 nmol/l
T1/2 7.5 h 12 h 54 h
Tau 24 h 24 h 72 h
Tmax 4 h 4 h 12 h
Cmax 1040 nmol/l 1340 nmol/l 2860 nmol/l
AUCtau 12500 h·nmol/l 23700 h·nmol/l 150000 h·nmol/l

Semaglutide/司美格鲁肽 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03707990 Obesity and Overweight Phase 1 Recruiting September 11, 2019 United States, Arizona ... 展开 >> Novo Nordisk Investigational Site Recruiting Tempe, Arizona, United States, 85283 收起 <<
NCT00851773 Diabetes Heal... 展开 >>thy 收起 << Phase 1 Completed - United Kingdom ... 展开 >> London SW, United Kingdom, 17 0RE 收起 <<
NCT01686945 Diabetes Diab... 展开 >>etes Mellitus, Type 2 Healthy 收起 << Phase 1 Completed - Germany ... 展开 >> Novo Nordisk Investigational Site Berlin, Germany, 14050 收起 <<

Semaglutide/司美格鲁肽 参考文献

[1]Lau J, Bloch P, et al. Discovery of the Once-Weekly Glucagon-Like Peptide-1 (GLP-1) Analogue Semaglutide. J Med Chem. 2015 Sep 24;58(18):7370-80.

[2]Zhang L, Zhang L, et al. Semaglutide is Neuroprotective and Reduces α-Synuclein Levels in the Chronic MPTP Mouse Model of Parkinson's Disease. J Parkinsons Dis. 2019;9(1):157-171.

[3]Rakipovski G, Rolin B, et al. The GLP-1 Analogs Liraglutide and Semaglutide Reduce Atherosclerosis in ApoE-/- and LDLr-/- Mice by a Mechanism That Includes Inflammatory Pathways. JACC Basic Transl Sci. 2018 Nov 21;3(6):844-857.

[4]Semaglutide

[5]Semaglutide

Semaglutide/司美格鲁肽 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

0.24mL

0.05mL

0.02mL

1.22mL

0.24mL

0.12mL

2.43mL

0.49mL

0.24mL

Semaglutide/司美格鲁肽 技术信息

CAS号910463-68-2
分子式C187H291N45O59
分子量 4113.58
SMILES Code CC[C@@H]([C@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC(CNC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC(CNC([C@@H](NC(C(C)(NC([C@@H](N)CC1=CN=CN1)=O)C)=O)CCC(O)=O)=O)=O)[C@H](O)C)=O)CC2=CC=CC=C2)=O)[C@H](O)C)=O)CO)=O)CC(O)=O)=O)C(C)C)=O)CO)=O)CO)=O)CC3=CC=C(O)C=C3)=O)CC(C)C)=O)CCC(O)=O)=O)=O)CCC(N)=O)=O)C)=O)C)=O)CCCCNC(COCCOCCNC(COCCOCCNC(CC[C@@H](NC(CCCCCCCCCCCCCCCCC(O)=O)=O)C(O)=O)=O)=O)=O)=O)CCC(O)=O)=O)CC4=CC=CC=C4)=O)C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(NCC(N[C@H](C(NCC(O)=O)=O)CCCNC(N)=N)=O)=O)CCCNC(N)=N)=O)C(C)C)=O)CC(C)C)=O)CC5=CNC6=CC=CC=C65)=O)C)=O)C
MDL No. N/A
别名 索马鲁肽;索玛鲁肽
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C
溶解方案

DMSO: 3 mg/mL(0.73 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 20 mg/mL(4.86 mM)，配合低频超声，并调节pH至1

Tags: Semaglutide | 910463-68-2 | GCGR | Glucagon Receptor | GLP-1R Agonist | GPCR/G Protein | GCGR | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Semaglutide/司美格鲁肽 纯度/质量文件 | Semaglutide/司美格鲁肽 生物活性 | Semaglutide/司美格鲁肽 动物研究 | Semaglutide/司美格鲁肽 临床数据 | Semaglutide/司美格鲁肽 参考文献 | Semaglutide/司美格鲁肽 实验方案 | Semaglutide/司美格鲁肽 技术信息

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