Semaglutide 索马鲁肽

Semaglutide 索马鲁肽;Liraglutide 利拉鲁肽; GLP-1受体激动剂;Metformin HCl 盐酸二甲双胍;Acarbose 阿卡波糖;Antidiabetic drug抗糖尿病药物;Streptozotocin (STZ) 链脲佐菌素;CAS:910463-68-2;

产品信息

产品名称

产品编号 CAS NO. 规格

Semaglutide 索马鲁肽

MZ7352-1MG 910463-68-2 1mg
Semaglutide 索马鲁肽 MZ7352-5MG 910463-68-2 5mg

Semaglutide 索马鲁肽 MZ7352-10MG 910463-68-2 10mg

索马鲁肽(Semaglutide)是一种胰高血糖素样肽-1(GLP-1) 受体激动剂,在表达人受体的BHK细胞报告基因实验中,EC50=6.2 pM。在db/db小鼠的II型糖尿病中,索马鲁肽可降低血糖水平,以葡萄糖依赖的方式刺激胰岛素和抑制胰高血糖素分泌。索马鲁肽是比利拉鲁肽(Liraglutide, MZ7351)更长效的替代物,结构上类似于GLP-1。在MPTP诱导的帕金森模型中,索马鲁肽(25 nmol/kg)预防塞梅林氏神经节中多巴胺能神经元的减少,提高塞梅林氏神经节和纹状体中的脂质过氧化,以及改善滚轴实验和足迹分析中动物的运动协调。索马鲁肽具抗肥胖活性。减低能量摄取,索马鲁肽诱导的体重减轻可能的作用机制包括:食欲降低,更好的控制饮食和相对来说更低程度的嗜好脂肪和热量较重的食物。

产品特性

1)CAS NO:910463-68-2

2) 序列:H-His-Aib-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala- Lys(AEEAc-AEEAc-γ-Glu-17-carboxyheptadecanoyl)-Glu-Phe-Ile-Ala-Trp-Leu-Val-Arg-Gly-Arg-Gly-OH

3) 同义名:Semaglutide free acid; NN 9535; NNC 0113-0217; Ozempic

4)分子式:C187H291N45O59

5) 分子量:4113.58

6) 纯度:≥98%

7) 外观:白色粉末

8) 溶解性:溶于DMSO(3mg/ml)、不溶于乙醇和水

保存与运输方法

保存:2-8℃密封干燥短期保存,长期置于-20℃密封干燥保存,至少2年有效。 

运输:冰袋运输。

注意事项

  • 针对溶解性比较差的化合物,可通过≤60℃温育和(或)超声的方式来促进其溶解。不同批次化合物的溶解性会有差异,以实际测定为准。
  • 本品配制的储存液请尽快使用,若单次不能用完,请根据单次用量分装,≤-20℃保存(-20℃一个月;-80℃ 六个月)。
  • 本品并非商业化的临床药物,仅用作科研用途,不得用作临床诊断或治疗,不得用于食品或药品,绝对禁止用在人身上。
  • 为了您的安全和健康,请穿实验服并戴一次性手套操作。

配制储存液

          质量

溶剂体积

浓度

1mg 5mg 10mg
0.5mM 0.4862 mL 2.4310 mL 4.8619 mL
0.1mM 2.4310 mL 12.1549 mL 24.3097mL

使用方法【源自文献,仅作参考】

文献1,Rakipovski G, Rolin B, Nøhr J, Klewe I, Frederiksen KS, Augustin R, Hecksher-Sørensen J, Ingvorsen C, Polex-Wolf J, Knudsen LB. 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. doi: 10.1016/j.jacbts.2018.09.004. PMID: 30623143; PMCID: PMC6314963.

体内研究(动物模型):

动物模型(Animal Model):C57BL/6J lean male mice at 12 weeks of age

实验方法(Assay):To study acute inflammation in vivo study design, C57BL/6J lean male mice at 12 weeks of age were given SC doses of semaglutide (60.0 μg/kg) or vehicle control 1 hour prior to receiving an IP dose of lipopolysaccharide (LPS) (0.05 mg/kg, Escherichia coli O55:B5) or vehicle control. Blood samples were collected from the sinus orbital vein at 1 and 4 h after LPS dose.

文献2, Wang L, Ding J, Zhu C, Guo B, Yang W, He W, Li X, Wang Y, Li W, Wang F, Wang F, 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 48: 219, 2021

体外研究:

细胞类型(Cell type):BV2 cells

实验方法(Assay): BV2 cells were seeded into 96-well plates (1×104 cells/well) for 12 h, and then treated with different doses (300, 600, 900 or 1,000 nM) of semaglutide for 20 h at 37°C. A blank well with culture medium was used to detect background, and five replicate wells were established per group. CCK-8 reagent (100 µl) was added to evaluate cellular proliferation.

体内研究(动物模型):

动物模型(Animal Model):C57BL/6J mice (male, 10±2 weeks old; weight, 25±3 g)

实验方法(Assay):The animals were randomized into five groups (20 per group), all of which were treated by intraperitoneal (i.p.) injection. In the control group (1% DMSO, i.p.), mice received 20 injections in total – 19 injections every other day for 37 days, and a final injection on the 45th day. For the semaglutide group [25 nM/kg semaglutide i.p.], the administration schedule was the same as that for the control group. In the PTZ group [37 mg/kg PTZ, i.p.], the mice received a total of 16 injections – one injection every other day from the 9th to the 37th day for a total of 15 injections, and a final injection on the 45th day. For the low-dose semaglutide group [37 mg/kg PTZ + 10 nM/kg semaglutide, i.p.], the semaglutide administration schedule was the same as that for the control group, and the PTZ administration schedule was the same as that for the PTZ group, 30 min after each injection of semaglutide. For the high-dose semaglutide group (37 mg/kg PTZ + 25 nM/kg semaglutide, i.p.), the administration schedule was the same as that for the low-dose semaglutide group.

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