Semaglutide
(Synonyms: 索马鲁肽) 目录号 : GC31404
Semaglutide是人胰高血糖素样肽-1的长效类似物,可作为人胰高血糖素样肽-1 (GLP-1)受体的激动剂。
Cas No.:910463-68-2
Sample solution is provided at 25 µL, 10mM.
Semaglutide is a long-acting analogue of human glucagon-like peptide-1 and an agonist for the human glucagon-like peptide-1 (GLP-1) receptor. It reduces blood sugar, body weight and blood pressure and improves blood sugar control in adults with type 2 diabetes[1-2].
Semaglutide(900 nM; 24h) attenuated the LPS‑ and nigericin‑induced inflammatory response and LDH release by blocking NLRP3 inflammasome activation in BV2 cells[3]. Semaglutide(5nM; 30min) promoted expression of GLP1R and activated PKG/PKCε/ERK1/2 signaling pathway in H/R H9C2 cells[4].
Semaglutide(40 µg/kg once every 3 days；4weeks；s.q) showed significant anti-inflammatory effects and mitigated the ER stress in eWAT adipocytes of obese mice[5]. Semaglutide(30 nmol/kg/day ;i.p; 12 weeks)reduces body weight, improves glucose metabolism, inflammation and oxidative stress in obese mice[6]. Semaglutide(0.1 mg/kg; i. p ) reduced blood glucose and promoted glucose metabolism in the brain of 3xTg mice via the SIRT1 pathway[7].
References:
[1]. FrÍas JP, Davies MJ, et, al. SURPASS-2 Investigators. Tirzepatide versus Semaglutide Once Weekly in Patients with Type 2 Diabetes. N Engl J Med. 2021 Aug 5;385(6):503-515. doi: 10.1056/NEJMoa2107519. Epub 2021 Jun 25. PMID: 34170647.
[2]. Chao AM, Tronieri JS, et, al. Semaglutide for the treatment of obesity. Trends Cardiovasc Med. 2023 Apr;33(3):159-166. doi: 10.1016/j.tcm.2021.12.008. Epub 2021 Dec 21. PMID: 34942372; PMCID: PMC9209591.
[3]. Wang L, Ding J, et, al. Semaglutide attenuates seizure severity and ameliorates cognitive dysfunction by blocking the NLR family pyrin domain containing 3 inflammasome in pentylenetetrazole‑kindled mice. Int J Mol Med. 2021 Dec;48(6):219. doi: 10.3892/ijmm.2021.5052. Epub 2021 Oct 22. PMID: 34676876; PMCID: PMC8547541.
[4]. Zhu Q, Luo Y, et, al. Semaglutide inhibits ischemia/reperfusion-induced cardiomyocyte apoptosis through activating PKG/PKCε/ERK1/2 pathway. Biochem Biophys Res Commun. 2023 Mar 5;647:1-8. doi: 10.1016/j.bbrc.2023.01.049. Epub 2023 Jan 17. PMID: 36706596.
[5]. Martins FF, Marinho TS, et, al. Semaglutide (GLP-1 receptor agonist) stimulates browning on subcutaneous fat adipocytes and mitigates inflammation and endoplasmic reticulum stress in visceral fat adipocytes of obese mice. Cell Biochem Funct. 2022 Dec;40(8):903-913. doi: 10.1002/cbf.3751. Epub 2022 Sep 28. PMID: 36169111.
[6]. Pan X, Yang L, et, al. Semaglutide ameliorates obesity-induced cardiac inflammation and oxidative stress mediated via reduction of neutrophil Cxcl2, S100a8, and S100a9 expression. Mol Cell Biochem. 2023 Jun 15. doi: 10.1007/s11010-023-04784-2. Epub ahead of print. PMID: 37318712.
[7]. Wang ZJ, Li XR, et, al. Semaglutide ameliorates cognition and glucose metabolism dysfunction in the 3xTg mouse model of Alzheimer's disease via the GLP-1R/SIRT1/GLUT4 pathway. Neuropharmacology. 2023 Dec 1;240:109716. doi: 10.1016/j.neuropharm.2023.109716. Epub 2023 Sep 18. PMID: 37730113.
Semaglutide是人胰高血糖素样肽-1的长效类似物,可作为人胰高血糖素样肽-1 (GLP-1)受体的激动剂。它可以降低血糖、体重和血压,改善成人2型糖尿病患者的血糖控制[1-2]。
Semaglutide(900 nM; 24h)通过阻断BV2细胞中NLRP3炎性体的激活,减弱LPS和尼日利亚菌素诱导的炎症反应和LDH释放[3]。Semaglutide(5nM; 30min)在H/R H9C2细胞中促进GLP1R的表达,激活PKG/PKCε/ERK1/2信号通路[4]。
Semaglutide (40 µg/kg once every 3 days; 4weeks; s.q)具有显著的抗炎作用,可减轻肥胖小鼠eWAT脂肪细胞内质网应激[5]。Semaglutide(30 nmol/kg/day ; i.p; 12 weeks) 减轻体重,改善肥胖小鼠的葡萄糖代谢,炎症和氧化应激[6]。Semaglutide (0.1 mg/kg; i. p) 通过SIRT1途径降低3xTg小鼠的血糖并促进脑内葡萄糖代谢[7]。
| Cell experiment [1]: | |
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Cell lines |
BV2 cells |
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Preparation Method |
Cells were assigned to four groups as follows: i) The control group, treated with 1% DMSO; ii) the semaglutide group, treated with 900 nM semaglutide; iii) the lipopolysaccharide (LPS) + nigericin group, treated with 1 µg/ml LPS and 10 µM nigericin; and iv) the semaglutide + LPS + nigericin group, treated with 900 nM semaglutide followed by 1 µg/ml LPS and 10 µM nigericin. |
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Reaction Conditions |
900 nM; 24h |
|
Applications |
Semaglutide inhibits LPS- and nigericin-mediated lactate dehydrogenase (LDH) release in BV2 cells. |
| Animal experiment [2]: | |
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Animal models |
C57BL/6 male mice |
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Preparation Method |
Normal mice and obese mice were randomly assigned to a diet plus Semaglutide or no Semaglutide. Semaglutide was administered subcutaneously to mice at 40 µg/kg once every 3 days (corresponding to 1.2 µg per animal). The stock semaglutide solution (1.34 mg/ml) was diluted in sterile 0.9% NaCl to 6.0 µg/ml so that an injection volume of 200 µl would contain 1.2 µg of the drug. Untreated groups were given sterile subcutaneous saline. |
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Dosage form |
40 µg/kg once every 3 days; 4weeks; s.q |
|
Applications |
Semaglutide stimulates browning on subcutaneous fat adipocytes and mitigates inflammation and endoplasmic reticulum stress in visceral fat adipocytes of obese mice. |
|
References: [1]. Wang L, Ding J, et, al. Semaglutide attenuates seizure severity and ameliorates cognitive dysfunction by blocking the NLR family pyrin domain containing 3 inflammasome in pentylenetetrazole‑kindled mice. Int J Mol Med. 2021 Dec;48(6):219. doi: 10.3892/ijmm.2021.5052. Epub 2021 Oct 22. PMID: 34676876; PMCID: PMC8547541. | |
| Cas No. | 910463-68-2 | SDF | |
| 别名 | 索马鲁肽 | ||
| Canonical SMILES | [Semaglutide] | ||
| 分子式 | 分子量 | 4113.58 | |
| 溶解度 | DMSO：3mg/mL (0.73 mM) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.2431 mL | 1.2155 mL | 2.431 mL |
| 5 mM | 0.0486 mL | 0.2431 mL | 0.4862 mL |
| 10 mM | 0.0243 mL | 0.1215 mL | 0.2431 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.50%
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