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Technical Data
| Formula | C27H36N2O4 |
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| Molecular Weight | 452.59 | CAS No. | 135062-02-1 | |
| Solubility (25°C)* | In vitro | DMSO | 91 mg/mL (201.06 mM) | |
| Ethanol | 91 mg/mL (201.06 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | Repaglinide (AG-EE 623 ZW) is a potassium channel blocker, which lowers blood glucose by stimulating the release of insulin from the pancreas, used the treatment of type II diabetes. | |
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| In vitro | 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. [1] 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. [2] 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. [3] | |
| In vivo | 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. [4] |
Protocol (from reference)
References
Selleck's Repaglinide has been cited by 1 publication
| Hepatic OATP-mediated clearance in the Beagle dog: assessing in vitro-in vivo relationships and applying cross species empirical scaling factors to improve prediction of human clearance [Matsunaga N Drug Metab Dispos, 2019, ;47(3):215-226] | PubMed: 30593544 |
RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.