产品说明书
Semaglutide
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同义名 : | 索马鲁肽;索玛鲁肽 |
| CAS号 : | 910463-68-2 | |
| 货号 : | A753934 | |
| 分子式 : | C187H291N45O59 | |
| 纯度 : | 99% | |
| 分子量 : | 4113.58 | |
| MDL号 : | N/A | |
| 存储条件： |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 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 |
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| 动物实验配方： |
| 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] | ||
| 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 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
0.24mL 0.05mL 0.02mL |
1.22mL 0.24mL 0.12mL |
2.43mL 0.49mL 0.24mL |
| 参考文献 |
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