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| 品牌 | absin | CAS | 135062-02-1 |
|---|---|---|---|
| 分子式 | C27H36N2O4 | 纯度 | 99% |
| 分子量 | 452.59 | 货号 | abs47027490 |
| 规格 | 50mg | 供货周期 | 现货 |
| 主要用途 | used for the treatment of non-insulin-de | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
Repaglinide 135062-02-1
| 产品描述 | |
| 描述 | Repaglinide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It belongs to the meglitinide class of short-acting insulin secretagogues, which act by binding to ? cells of the pancreas to stimulate insulin release. Repaglinide induces an early insulin response to meals decreasing postprandial blood glucose levels. It should only be taken with meals and meal-time doses should be skipped with any skipped meal. Approximately one month of therapy is required before a decrease in fasting blood glucose is seen. Meglitnides may have a neutral effect on weight or cause a slight increase in weight. The average weight gain caused by meglitinides appears to be lower than that caused by sulfonylureas and insulin and appears to occur only in those na?ve to oral antidiabetic agents. Due to their mechanism of action, meglitinides may cause hypoglycemia although the risk is thought to be lower than that of sulfonylureas since their action is dependent on the presence of glucose. In addition to reducing postprandial and fasting blood glucose, meglitnides have been shown to decrease glycosylated hemoglobin (HbA1c) levels, which are reflective of the last 8-10 weeks of glucose control. Meglitinides appear to be more effective at lowering postprandial blood glucose than metformin, sulfonylureas and thiazolidinediones. Repaglinide is extensively metabolized in the liver and excreted in bile. Repaglinide metabolites do not possess appreciable hypoglycemic activity. Approximately 90% of a single orally administered dose is eliminated in feces and 8% in urine. |
| 纯度 | 99% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | 瑞ge列奈；AG-EE 623ZW |
| 外观 | 白色结晶性粉末 |
| 可溶性/溶解性 | DMSO : 84 mg/mL (185.6 mM) Ethanol : 84 mg/mL (185.6 mM) |
| 生物活性 | |
| 靶点 | Potassium channel |
| In vitro(体外研究) | Repaglinide is found to bind with low affinity (K(D)=59 nM) to SUR1 alone, but with high affinity (increased approximately 150-fold) when SUR1 is co-expressed with Kir6.2. Repaglinide binds with low affinity (K(D)=51 nM) to SUR1 co-expressed with Kir6.2DeltaN14. Repaglinide lowers the plasma glucose concentration in the control rat, whilst failing to affect significantly the plasma insulin concentration or insulin/glucose ratio. Repaglinide administration affects neither plasma glucose nor insulin concentration, restores a normal value for the otherwise abnormally high basal insulin output, increases the 16.7 mM/2.8 mM ratio for insulin release, and again augmented protein biosynthesis at both low and high hexose concentrations in Goto-Kakizaki (GK) rats. Repaglinide is found to bind to NCS proteins, but not to CaM or S100 proteins, in a Ca2+-dependent manner. Repaglinide antagonizes the inhibitory action of recoverin in a rhodopsin kinase assay with IC50 values of 400 mM. Repaglinide tightly binds to the visinin-like domain of CCaMK and PpCaMK in a Ca2+-dependent manner and antagonizes the regulatory function of the domain with IC50 values of 55 and 4 mM for CCaMK and PpCaMK respectively. |
| In vivo(体内研究) | Repaglinide provokes a greater and more rapid increase in plasma insulin concentration and an earlier fall in glycemia than those observed after administration of the hypoglycemic sulfonylureas in both fed and starved normal rats. |
| 参考文献 | |
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| 研究领域 | |
| 研究领域 | Metabolism CancerCancer Metabolism Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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