RO-28-1675

SKU: orb1706690

Description

RO-28-1675 is a direct glucokinase activator whose efficacy inversely correlates with glucose levels. It is a research tool for studying insulin secretion mechanisms and has been utilized in both in vitro and in vivo models of type 2 diabetes.

Research Area

Metabolism Research

Key Properties

• CAS Number: 300353-13-3
• MW: 378.51
• Purity: 98.13% (May vary between batches)
• Formula: C₁₈H₂₂N₂O₃S₂
• SMILES: [C@@H](C(NC1=NC=CS1)=O)(CC2CCCC2)C3=CC=C(S(C)(=O)=O)C=C3
• Target: Glucokinase
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.28 mM);DMSO:40 mg/mL (105.68 mM)

Bioactivity

• Target IC50:
  GK:54 nM (EC50)
• In Vivo:
  In a diabetic mouse model with a Gck gene mutation, oral administration of RO-28-1675 (50 mg/kg) induced hypoglycemia in wild-type mice . Pharmacokinetic studies indicated that RO-28-1675 has excellent absorption properties, with an oral bioavailability of 92.8% in mice. After a single dose of 10 mg/kg, the peak plasma concentration (Cmax) reached 1140 μg/mL .
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• In Vitro:
  In experiments with rat islet (Langerhans islet) cells and primary rat hepatocytes, RO-28-1675 showed an effect on the nuclear-cytoplasmic transport of glucokinase (GCK) in hepatocytes. Additionally, RO-28-1675 (3 μM) was able to lower the glucose concentration threshold required to stimulate insulin secretion. This suggests that RO-28-1675 not only regulates the subcellular localization of GCK but also enhances the glucose sensitivity of islet cells, thereby promoting insulin secretion .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

RO 28 1675, Ro 28-1675, RO281675, RO-28-1675, Ro28-1675

Compound Identifiers

PubChem CID

9886086