Glimepiride (Hoe 490) is a new sulfonylurea. After oral administration of Hoe 490 to rabbits, blood glucose was lowered 3.5 times more than after glibenclamide (HB 419) and after intravenous administration, 2.5 times more. The more rapid decrease in blood glucose in the dog after oral administration of glimepiride was accompanied by a correspondingly earlier and higher plasma insulin increase[3]. Glimepiride is a second-generation sulfonylurea that stimulates pancreatic β cells to release insulin. It can also be combined with other antihyperglycemic agents, including metformin and insulin, in patients who are not adequately controlled by sulfonylureas alone[4]. Glimepiride decreased extracellular Aβ40 and Aβ42 levels. The effect of glimepiride on reduction of Aβ40 generation was mediated by downregulation of β-site APP-cleaving enzyme 1 (BACE1) mRNA and protein expression, and by suppression of BACE1 activity[5].
Glimepiride/格列美脲 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Microglial cells
5 μM
1 hour
Glimepiride reduced cellular CD14 expression and cytokine secretion in microglial cells
J Neuroinflammation. 2014 Jun 21;11:115
RAW 264 cells
5 μM
1 hour
Glimepiride stimulated the release of CD14 from RAW 264 cells and reduced cytokine secretion
J Neuroinflammation. 2014 Jun 21;11:115
Primary human white preadipocytes
2.5 μM
21 days
To evaluate the effect of glimepiride on adipogenesis, results showed that glimepiride significantly increased adipogenesis, but the effect was lower than glibenclamide and rosiglitazone
Mol Metab. 2024 Jul;85:101956
HEK293T cells
10 μM
24 hours
To evaluate the effect of glimepiride on PPARγ transcriptional activity, results showed that glimepiride only weakly increased reporter activity
Mol Metab. 2024 Jul;85:101956
Kir6.2 DC36 channels
300 μM
To study the inhibitory effect of glimepiride on Kir6.2 DC36 channels, it was found to inhibit currents via a low-affinity site
Br J Pharmacol. 2001 May;133(1):193-9
Xenopus oocytes
3.0 nM (SUR1), 5.4 nM (SUR2A), 7.3 nM (SUR2B)
To investigate the inhibitory effect of glimepiride on recombinant KATP channels, it was found to inhibit Kir6.2/SUR1, Kir6.2/SUR2A, and Kir6.2/SUR2B currents via high-affinity and low-affinity sites
Br J Pharmacol. 2001 May;133(1):193-9
U-87MG malignant glioma cells
1.56 µM
3 hours
Combination with DOXO significantly increased intracellular DOXO levels
Int J Mol Sci. 2025 Feb 8;26(4):1429
HepG2 liver cancer cells
1.56 µM
3 hours
Combination with DOXO significantly increased intracellular DOXO levels
Int J Mol Sci. 2025 Feb 8;26(4):1429
A549 lung cancer cells
1.56 µM
3 hours
Combination with DOXO increased intracellular DOXO levels by 227%
Int J Mol Sci. 2025 Feb 8;26(4):1429
MCF-7 breast cancer cells
45.1 µM
72 hours
Combination with DOXO reduced cell viability to 16.0% compared to 70.2% for DOXO alone, showing a 4.4-fold increase in cytotoxicity
Int J Mol Sci. 2025 Feb 8;26(4):1429
GSC11 cells
1 μM
Glimepiride significantly increased CLIP3 expression and reduced NANOG and OCT4 expression.
J Exp Clin Cancer Res. 2021 Sep 6;40(1):282
T98G cells
1 μM
48 hours
Evaluated the effect of glimepiride on T98G cell viability, showing that IR significantly improved glimepiride sensitivity.
J Exp Clin Cancer Res. 2021 Sep 6;40(1):282
U87MG cells
1 μM
48 hours
Evaluated the effect of glimepiride on U87MG cell viability, showing that IR significantly improved glimepiride sensitivity.
J Exp Clin Cancer Res. 2021 Sep 6;40(1):282
Glimepiride/格列美脲 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57Bl/6N mice
High-fat diet-induced obese mice
Intraperitoneal injection
10 mg/kg
Twice daily for 6 days
To evaluate the effect of glimepiride on PPARγ Ser-273 phosphorylation, results showed that glimepiride reduced PPARγ phosphorylation in white adipose tissue and increased UCP1 expression
Mol Metab. 2024 Jul;85:101956
Mice
High-fat diet-induced type 2 diabetic model
Oral
2 mg/kg body weight/day
Once daily for 7 weeks
To compare the antistroke efficacy of glimepiride with linagliptin in type 2 diabetic mice. Results showed that glimepiride was efficacious against stroke in normal mice only, not in diabetic mice.
Diabetes. 2013 Apr;62(4):1289-96
Mice
High-fat diet-induced type 2 diabetes model
Oral (in food)
2-4 mg/kg body weight per day
Once daily for 3 months
To evaluate the reversal effect of glimepiride on type 2 diabetes-induced brain microvascular pathology. Results showed that glimepiride enhanced angiogenesis, increased pericyte density, restored BBB integrity, and reduced microglial activation.
Diabetes. 2023 Mar 1;72(3):405-414
BALB/c mice
4T1 breast cancer model
Intraperitoneal and intravenous
4 mg/kg
Administered on days 9, 11, 14, 17, and 21, totaling 5 times
Tumor volume in the combination group was 35% smaller than in the DOXO-only group and 72% smaller than in the control group, but the combination therapy group experienced a 13% greater body weight loss
Int J Mol Sci. 2025 Feb 8;26(4):1429
Rabbits
GCK-NFS rabbit model
Oral
0.2 mg/kg
Once daily for 28 days
Glimepiride significantly reduced fasting blood glucose levels and improved islet function in GCK-NFS rabbits.
Cell Mol Life Sci. 2020 Aug;77(16):3265-3277
BALB/c nude mice
Intracranial GBM xenograft model
Oral
5 mg/kg
Once daily for 5 days
Combination of glimepiride with IR significantly inhibited tumor growth and improved survival.
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