| Name | Repaglinide |
| Description | Repaglinide (AG-EE 623ZW) is a benzoic acid derivative that stimulates insulin secretion from the pancreas and is used in the therapy of type 2 diabetes. Repaglinide has been linked to rare instances of clinically apparent acute liver injury. |
| In vitro | Repaglinide binds to NCS proteins in a calcium-dependent manner, but does not bind to CAM or S100 proteins.Repaglinide tightly binds to CCaMK and PpCaMK in a calcium-dependent manner, antagonizing the regulatory function of the structural domains, with IC 50 values of 55 mM and 4 mM for the CCaMK and PpCaMK domains.Repaglinide binds to CCaMK and PpCaMK domains with low affinity (K(D) = 59 nM) to bind SUR1 alone, but binds SUR1 with high affinity to co-express with Kir6.2, increasing it approximately 150-fold.Repaglinide antagonizes the inhibitory effect of restoring protein in the retinal kinase assay, with an IC50 value of 400 mM.Repaglinide also antagonizes the inhibitory effect of restoring protein in the retinal kinase assay, with an IC50 value of 400 mM. |
| In vivo | Repaglinide binds to NCS proteins in a calcium-dependent manner, but does not bind to CAM or S100 proteins.Repaglinide tightly binds to CCaMK and PpCaMK in a calcium-dependent manner, antagonizing the regulatory function of the structural domains, with IC 50 values of 55 mM and 4 mM for the CCaMK and PpCaMK domains.Repaglinide binds to CCaMK and PpCaMK domains with low affinity (K(D) = 59 nM) to bind SUR1 alone, but binds SUR1 with high affinity to co-express with Kir6.2, increasing it approximately 150-fold.Repaglinide antagonizes the inhibitory effect of restoring protein in the retinal kinase assay, with an IC50 value of 400 mM.Repaglinide also antagonizes the inhibitory effect of restoring protein in the retinal kinase assay, with an IC50 value of 400 mM. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | Ethanol : 84 mg/mL (185.6 mM), Sonication is recommended. DMSO : 250 mg/mL (552.38 mM), Sonication is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble) 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.42 mM), Sonication is recommended.
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| Keywords | type-2 | secretagogue | Repaglinide | PPARγ | PotassiumChannel | Potassium Channel | mellitus. | insulin | Inhibitor | inhibit | diabetes | CMBA | carbamoylmethyl | benzoic | acid |
| Inhibitors Related | PHYTOL | Minoxidil sulfate | Rosiglitazone | Daidzein | Hydrochlorothiazide | 1,8-Cineole | Maltitol | 2,3-Butanediol | NPC 15199 | Chlorzoxazone | Cloxiquine | Indapamide |
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