Aleglitazar

SKU: orb1707695

Description

Aleglitazar (R1439) is a dual agonist of PPARα and PPARγ with IC50 values of 38 nM and 19 nM, respectively. It has been investigated in preclinical research for type 2 diabetes, including studies on glycemic control and lipid metabolism in vitro and in animal models.

Research Area

Metabolism Research, Molecular Biology

Key Properties

• CAS Number: 475479-34-6
• MW: 437.51
• Purity: 99.42% (May vary between batches)
• Formula: C₂₄H₂₃NO₅S
• SMILES: C([C@@H](C(O)=O)OC)C1=C2C(=C(OCCC=3N=C(OC3C)C4=CC=CC=C4)C=C1)C=CS2
• Target: PPAR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.57 mM);DMSO:45 mg/mL (102.85 mM)

Bioactivity

• Target IC50:
  PPARα:38 nM|PPARγ:19 nM
• In Vivo:
  Aleglitazar (0.3-3.0 mg/kg; i.p.; daily; for 7 days) exerts beneficial effects on structural and functional outcomes of mild brain ischemia, reduces key aspects of microglia activation including NO production, release of proinflammatory cytokines, migration, and phagocytosis, and attenuates inflammatory responses in the post-ischemic brain.
• In Vitro:
  Aleglitazar exhibits species selectivity for PPARα, with EC50 values of 50 nM, 2.26 μM, and 2.34 μM for human, rat, and mouse PPARα, respectively. At concentrations of 0.01-40 μM (12-48 hours), aleglitazar does not significantly increase lactate dehydrogenase (LDH) release at 0.1-20 μM but shows significant increases at 30 μM and 40 μM. Additionally, aleglitazar (0.01-20 μM; 48 hours) decreases hyperglycemia (HG, glucose 25 mM)-induced apoptosis, caspase-3 activity, and cytochrome-C release, while improving cell viability in hyperglycemic conditions.

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

R1439, R-1439, PPARα, PPARγ, R 1439, RO0728804, RO-0728804, RO 0728804, Aleglitazar

Compound Identifiers

PubChem CID

10274777