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Glimepiride(Glimperide HOE-490)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Glimepiride(Glimperide HOE-490)图片
CAS NO:93479-97-1
规格:≥98%
包装与价格:
包装价格(元)
250mg电议
500mg电议
1g电议
2g电议
10g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)490.62
FormulaC24H34N4O5S
CAS No.93479-97-1
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 11 mg/mL (22.4 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Other info

Chemical Name: 4-ethyl-3-methyl-N-[2-[4-[(4-methylcyclohexyl)carbamoylsulfamoyl]phenyl]ethyl]-5-oxo-2H-pyrrole-1-carboxamide

InChi Key: WIGIZIANZCJQQY-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H34N4O5S/c1-4-21-17(3)15-28(22(21)29)24(31)25-14-13-18-7-11-20(12-8-18)34(32,33)27-23(30)26-19-9-5-16(2)6-10-19/h7-8,11-12,16,19H,4-6,9-10,13-15H2,1-3H3,(H,25,31)(H2,26,27,30)

SMILES Code: CCC1=C(CN(C1=O)C(=O)NCCC2=CC=C(C=C2)S(=O)(=O)NC(=O)NC3CCC(CC3)C)C

Synonyms

HOE-490; Glimepiride; HOE 490; HOE-490; Amaryl; Glimepiridum; Amarel; Glimepirida; Roname

实验参考方法
In Vitro

In vitro activity: 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). Glimepiride 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. Glimepiride associates in a time- and concentration dependent non-saturable manner with detergent-insoluble complexes of the plasma membrane which may correspond to caveolae. Glimepiride 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. Glimepiride 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.


Cell Assay: When cultured cells in the presence of a physiological insulin dose and glimepiride (10 μM), 2-deoxyglucose uptake was increased to 186% of control. Glimepiride also increased 2-deoxyglucose uptake in the absence of insulin. At the same time, glimepiride increased the expression of both GLUT1 and GLUT4 to 164% and 148% of control, respectively. These results suggested glimepiride increased cardiac glucose uptake in an insulin-independent pathway.

In VivoGlimepiride prevents the NA-STZ induced increased frequency of micronucleus (MN) in polychromatic and normochromatic erythrocytes. Glimepiride also decreases the sperm shape abnormality and enhances the sperm count besides improving the antioxidant status in the diabetic rats. Glimepiride inhibits the NA-STZ mediated changes in the MN frequency and sperm abnormality and enhanced the antioxidant defense. In diabetic-prone (DP) BB rats, Glimepiride (200 mg/kg/day) reduced the incidence of diabetes by 23% compared with the control group. In the hyperinsulinemic hyperglycemic KK-Ay mice, glimepiride reduced blood glucose by 40%, HBA1c by 33% and plasma insulin by 50%. In the absence of insulin, glimepiride caused glucose transport up to 60% and 35% of the maximum insulin response in the rat diaphragm and in 3T3 adipocytes, respectively.
Animal modelRats
Formulation & Dosage200 mg/kg
References

Br J Pharmacol. 2001 May;133(1):193-9; Horm Metab Res. 1996 Sep;28(9):469-87; Indian J Exp Biol. 2009 Oct;47(10):804-10.