research use only
Cat.No.S1344
| Related Targets | CFTR CRM1 CD markers AChR Calcium Channel Sodium Channel GABA Receptor TRP Channel ATPase GluR |
|---|---|
| Other Potassium Channel Inhibitors | Nigericin TRAM-34 Nicorandil ML133 HCl Hydralazine HCl Sophocarpine Senicapoc (ICA-17043) Gliquidone Butamben PAP-1 |
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In vitro |
DMSO
: 11 mg/mL
(22.42 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
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Working concentration: mg/ml;
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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| Molecular Weight | 490.62 | Formula | C24H34N4O5S |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 93479-97-1 | Download SDF | Storage of Stock Solutions |
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| Synonyms | HOE-490 | SMILES | CCC1=C(CN(C1=O)C(=O)NCCC2=CC=C(C=C2)S(=O)(=O)NC(=O)NC3CCC(CC3)C)C | ||
Read more about storage stability stock solution CAS number SMILES
| Targets/IC50/Ki |
SUR1
3 nM
SUR2A
5.4 nM
SUR2B
7.3 nM
|
|---|---|
| In vitro |
Glimepiride inhibits Kir6.2/SUR currents by interaction with two sites: a low-affinity site on Kir6.2 (IC(50)= approximately 400 mM) and a high-affinity site on SUR (IC(50)=3.0 nM for SUR1, 5.4 nM for SUR2A and 7.3 nM for SUR2B). This compound exhibits a higher potency compared to Glibenclamide with respect to stimulation of glucose transport, glucose transporter isoform 4 (GLUT4) translocation and lipid and glycogen synthesis in normal and insulin-resistant adipocytes and in muscle cells, as well as of the potential underlying signalling processes examined at the molecular level. It associates in a time- and concentration dependent non-saturable manner with detergent-insoluble complexes of the plasma membrane which may correspond to caveolae. This chemical blocks pinacidil-activated whole-cell K(ATP) currents of cardiac myocytes with an IC(50) of 6.8 nM, comparable to the potency of Glibenclamide in these cells. It blocks K(ATP) channels formed by co-expression of Kir6.2/SUR2A subunits in HEK 293 cells in outside-out excised patches with a similar IC(50) of 6.2 nM. |
| In vivo |
Glimepiride prevents the NA-STZ induced increased frequency of micronucleus (MN) in polychromatic and normochromatic erythrocytes. This compound also decreases the sperm shape abnormality and enhances the sperm count besides improving the antioxidant status in the diabetic rats. It inhibits the NA-STZ mediated changes in the MN frequency and sperm abnormality and enhanced the antioxidant defense. |
References |
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(data from https://clinicaltrials.gov, updated on 2025-12-17)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT07288749 | NOT_YET_RECRUITING | Type 2 Diabetes Mellitus (T2DM); Chronic Heart Failure (CHF) |
Tongji Hospital |
2026-01-01 | PHASE3 |
| NCT07589387 | NOT_YET_RECRUITING | Diabete Mellitus |
Washington University School of Medicine |
2026-05-01 | |
| NCT07365358 | NOT_YET_RECRUITING | Diabete Type 2 |
Chong Kun Dang Pharmaceutical |
2026-03 | PHASE4 |
| NCT05975528 | UNKNOWN | Diabetes Mellitus; Cellular Senescence; Sodium-Glucose Transporter 2 Inhibitors |
Yonsei University |
2023-06-01 | PHASE4 |
| NCT06759922 | COMPLETED | Type 2 Diabetes Mellitus |
Bahria University |
2025-01-01 | PHASE4 |
| NCT06068686 | COMPLETED | Type 2 Diabetes |
Damanhour University |
2022-10-01 |
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