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

货号：A753934 同义名： 索马鲁肽;索玛鲁肽

Semaglutide is an analog of human GLP-1 with long-acting effect over the other GLP-1Ras.

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

货号：A753934 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]
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• BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]
• J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]
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Semaglutide 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 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 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 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 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 技术信息

CAS号910463-68-2
分子式C187H291N45O59
分子量 4113.58
别名 索马鲁肽;索玛鲁肽
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
溶解度

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
动物实验配方

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 纯度/质量文件 | Semaglutide 生物活性 | Semaglutide 动物研究 | Semaglutide 临床数据 | Semaglutide 参考文献 | Semaglutide 实验方案 | Semaglutide 技术信息

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