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Glimepiride (Synonyms: HOE 490)

Catalog No.GC10104 Copy One-Click Copy Product Info

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.

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Glimepiride Chemical Structure

Cas No.: 93479-97-1

Size Price Stock Qty
10mM (in 1mL DMSO)
$39.00
In stock
500mg
$35.00
In stock
1g
$59.00
In stock
5g
$200.00
In stock

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Sample solution is provided at 25 µL, 10mM.



Description of Glimepiride

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.

Protocol of Glimepiride

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:
[1] 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.
[2] 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.

Chemical Properties of Glimepiride

Cas No. 93479-97-1 SDF
Synonyms HOE 490
Chemical Name 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
Formula C24H34N4O3S M.Wt 490.62
Solubility ≥ 21.45 mg/mL in DMSO Storage Store at -20°C,dry,protect from light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Glimepiride

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.0382 mL 10.1912 mL 20.3824 mL
5 mM 407.6 μL 2.0382 mL 4.0765 mL
10 mM 203.8 μL 1.0191 mL 2.0382 mL
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In vivo Formulation Calculator (Clear solution) of Glimepiride

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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