Repaglinide

SKU: orb1309813

Description

Repaglinide is a benzoic acid-derived insulin secretagogue used to treat type 2 diabetes. It is a valuable research tool for studying pancreatic beta-cell function and glucose metabolism in both in vitro and in vivo experimental models. Rare cases of drug-induced liver injury have been associated with its clinical use.

Research Area

Metabolism Research, Molecular Biology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 135062-02-1
• MW: 452.59
• Purity: 99.73%
• Formula: C₂₇H₃₆N₂O₄
• SMILES: [C@H](NC(CC1=CC(OCC)=C(C(O)=O)C=C1)=O)(CC(C)C)C2=C(C=CC=C2)N3CCCCC3
• Target: Potassium Channel,PPAR
• Solubility: DMSO:250 mg/mL (552.38 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:84 mg/mL (185.6 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.42 mM)

Bioactivity

• 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

secretagogue, PotassiumChannel, Potassium Channel, PPARγ, Repaglinide, type-2, inhibit, mellitus., Inhibitor, insulin, diabetes, CMBA, benzoic, carbamoylmethyl, acid, AG-EE 388 ZW, AG-EE 623ZW

Compound Identifiers

PubChem CID

65981