Glimepiride
(Synonyms: 格列美脲; Glimperide; HOE-490) 目录号 : GC10104
Glimepiride为第二代磺酰脲类药物，可刺激胰岛β细胞释放胰岛素，作为单药或与二甲双胍、胰岛素联合用于治疗2型糖尿病。
Cas No.:93479-97-1
Sample solution is provided at 25 µL, 10mM.
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Glimepiride is a second-generation sulfonylurea that stimulates pancreatic β cells to release insulin. Glimepiride is used for the treatment of type 2 diabetes mellitu as monotherapy as well as in combination with metformin or insulin[1].
In vitro, Glimepiride (0, 0.3, 0.6, 1.2, 2.5 and 5μM; 1h) stimulated the release of CD14 from RAW 264 cells[2]. Glimepiride (10μM; 1, 4 and 7 days) induced the proliferation and differentiation of rat osteoblasts in a high glucose microenvironment[3]. Glimepiride (10µM; 30min) induces NO production by HCAECs[4].
In vivo, Glimepiride (1, 2 or 4mg/kg; 4 days; p.o.) prevents 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine induced dopamine neurons degeneration through attenuation of glia activation and oxidative stress in mice[5]. Glimepiride (4mg/kg; 3 weeks; i.p.) ameliorates renal toxicity induced by cadmium in mice[6].
References:
[1] Basit A, Riaz M, Fawwad A. Glimepiride: evidence-based facts, trends, and observations (GIFTS). [corrected]. Vasc Health Risk Manag. 2012;8:463-72.
[2] Ingham V, Williams A, Bate C. Glimepiride reduces CD14 expression and cytokine secretion from macrophages. J Neuroinflammation. 2014 Jun 21;11:115.
[3] Ma P, Gu B, Xiong W, Tan B, Geng W, Li J, Liu H. Glimepiride promotes osteogenic differentiation in rat osteoblasts via the PI3K/Akt/eNOS pathway in a high glucose microenvironment. PLoS One. 2014 Nov 12;9(11):e112243.
[4] Ueba H, Kuroki M, Hashimoto S, Umemoto T, Yasu T, Ishikawa SE, Saito M, Kawakami M. Glimepiride induces nitric oxide production in human coronary artery endothelial cells via a PI3-kinase-Akt dependent pathway. Atherosclerosis. 2005 Nov;183(1):35-9.
[5] Oduola-Akande MD, Ishola IO, Olubodun-Obadun TG, Akande AJ, Adeyemi OO. Glimepiride Prevents 1-Methyl-4-Phenyl-1,2,3,6-Tetrahydropyridine Induced Dopamine Neurons Degeneration Through Attenuation of Glia Activation and Oxidative Stress in Mice. Neurotox Res. 2023 Jun;41(3):212-223.
[6] ElMahdy MK, Zaki MO, Al-Karmalawy AA, Abdo W, Alnasser SM, Antar SA. Glimepiride ameliorates renal toxicity induced by cadmium in mice: Modulation of Jun N terminal kinase (JNK)/nuclear factor kappa B (NF-κB) and phosphatidylinositol 3-kinases (PI3K)/protein kinase (AKT) pathways. Life Sci. 2022 Dec 15;311(Pt B):121184.
Glimepiride为第二代磺酰脲类药物，可刺激胰岛β细胞释放胰岛素，作为单药或与二甲双胍、胰岛素联合用于治疗2型糖尿病[1]。
体外实验显示，Glimepiride (0, 0.3, 0.6, 1.2, 2.5和5μM; 1h)可促进RAW264细胞CD14脱落[2]。在高糖微环境中，Glimepiride (10μM; 1, 4和7天)诱导大鼠成骨细胞增殖与分化[3]。Glimepiride (10μM; 30min)亦能诱导人冠状动脉内皮细胞(HCAECs)产生一氧化氮[4]。
体内研究证实，Glimepiride (1, 2或4mg/kg; 4天; 口服)可通过减弱胶质细胞活化及氧化应激预防1-甲基-4-苯基-1,2,3,6-四氢吡啶诱导的小鼠多巴胺神经元变性[5]。此外，Glimepiride (4mg/kg; 3周; 腹腔注射)可减轻镉诱导的小鼠肾毒性[6]。
| Cell experiment [1]: | |
Cell lines | HCAECs |
Preparation Method | HCAECs were incubated with 10µM Glimepiride, HGF (positive control) or vehicle in Krebs’ buffer (118mM NaCl, 4.7mM KCl, 2.5mM CaCl₂, 1.2mM MgSO₄, 1.2mM KH₂PO₄, 11mM glucose, 25mM NaHCO₃, 20mM HEPES, pH 7.4) pre-warmed to 37°C; after 30min the supernatant was collected from the dishes and kept at 4°C. The released nitric oxide (NO) was quantified within 24h of each collection using a NOx-analyzing HPLC system. |
Reaction Conditions | 10µM; 30min |
Applications | Glimepiride induces NO production by HCAECs. |
| Animal experiment [2]: | |
Animal models | 20 to 25g mice |
Preparation Method | During the experimental period, animals had ad libitum access to food and water; they were divided into four groups: Group 1 received saline as the normal control, Group 2 received intraperitoneal CdCl₂ (6.5mg/kg) for seven consecutive days as the CdCl₂ control, Group 3 received Glimepiride (4mg/kg; i.p.), and Group 4 was co-treated with CdCl₂ plus Glimepiride, with Glimepiride continued for 3 weeks. Twenty-four hours after the last dose, mice were anaesthetized with thiopental sodium (50mg/kg) and euthanized; blood collected via cardiac puncture into dry Eppendorf tubes was allowed to clot for 30min and then centrifuged at 2000g for 15min, and the serum was stored at -20°C for biochemical assays; both kidneys were excised—one fixed in 10% paraformaldehyde for histopathology and the other snap-frozen at -80°C for ELISA. |
Dosage form | 4mg/kg; 3 weeks; i.p. |
Applications | Glimepiride ameliorates renal toxicity induced by cadmium in mice. |
References: | |
| Cas No. | 93479-97-1 | SDF | |
| 别名 | 格列美脲; Glimperide; HOE-490 | ||
| 化学名 | 4-ethyl-3-methyl-N-[2-[4-[(4-methylcyclohexyl)carbamoylsulfamoyl]phenyl]ethyl]-5-oxo-2H-pyrrole-1-carboxamide | ||
| Canonical SMILES | CCC1=C(CN(C1=O)C(=O)NCCC2=CC=C(C=C2)S(=O)(=O)NC(=O)NC3CCC(CC3)C)C | ||
| 分子式 | C24H34N4O3S | 分子量 | 490.62 |
| 溶解度 | ≥ 21.45 mg/mL in DMSO | 储存条件 | Store at -20°C,dry,protect from light |
| 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 | 2.0382 mL | 10.1912 mL | 20.3824 mL |
| 5 mM | 0.4076 mL | 2.0382 mL | 4.0765 mL |
| 10 mM | 0.2038 mL | 1.0191 mL | 2.0382 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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