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Chemical Structure| 93479-97-1 Chemical Structure| 93479-97-1

Structure of Glimepiride
CAS No.: 93479-97-1

Chemical Structure| 93479-97-1

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Glimepiride is a sulfonylurea which inhibit KATP with IC50 of 3.0 nM in pancreatic β-cells with fewer cardiac actions. It is used in the treatment of type 2 diabetes mellitus.

Synonyms: Glimperide; HOE-490; Roname

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Product Details of Glimepiride

CAS No. :93479-97-1
Formula : C24H34N4O5S
M.W : 490.62
SMILES Code : O=C(N1C(C(CC)=C(C)C1)=O)NCCC2=CC=C(S(=O)(NC(N[C@H]3CC[C@H](C)CC3)=O)=O)C=C2
Synonyms :
Glimperide; HOE-490; Roname
MDL No. :MFCD00878417
InChI Key :WIGIZIANZCJQQY-UHFFFAOYSA-N
Pubchem ID :3476

Safety of Glimepiride

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • Potassium Channel

    SUR2B, IC50:7.3 nM

    SUR1, IC50:5.4 nM

In Vitro:

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

In Vivo:

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. J Exp Clin Cancer Res. 2021 Sep 6;40(1):282

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT05538819 Chronic Heart Failure|Type 2 D... More >>iabetes|Cardiovascular Mortality|Cohort Study Less << COMPLETED 2022-07-01 Tongji Hospital, Wuhan, Hubei,... More >> 430030, China Less <<
NCT00044447 Diabetes Mellitus, Non-Insulin... More >>-Dependent Less << PHASE3 COMPLETED 2025-09-02 Dallas Diabetes & Endocrine Ce... More >>nter, Dallas, Texas, 75230, United States Less <<
NCT01052909 Healthy PHASE1 COMPLETED 2025-12-03 Anapharm Inc, Sainte-Foy, Queb... More >>ec, GIV 2KB, Canada Less <<
NCT00437554 Diabetes Mellitus, Type 2 PHASE3 COMPLETED 2025-07-07 Handok, Seoul, Korea, Republic... More >> of Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.04mL

0.41mL

0.20mL

10.19mL

2.04mL

1.02mL

20.38mL

4.08mL

2.04mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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