Arhalofenate

SKU: orb1308055

Description

Arhalofenate (JNJ 39659100) is a selective partial PPARγ agonist developed for type 2 diabetes research. It has been investigated in both in vitro assays and in vivo models for its potential to improve glycemic control and insulin sensitization.

Research Area

Metabolism Research, Molecular Biology

Key Properties

• CAS Number: 24136-23-0
• MW: 415.79
• Purity: 99.62% (May vary between batches)
• Formula: C₁₉H₁₇ClF₃NO₄
• SMILES: [C@H](OC1=CC(C(F)(F)F)=CC=C1)(C(OCCNC(C)=O)=O)C2=CC=C(Cl)C=C2
• Target: PPAR
• Solubility: DMSO:132.5 mg/mL (318.67 mM)

Bioactivity

• In Vivo:
  MBX-102 significantly reduces fasting blood glucose, confirming that Arhalofenate (MBX 102) is an efficacious antidiabetic agent. Arhalofenate (60 mg/kg) causes a dramatic decrease in plasma and also results in a dose-dependent, significant decrease in the insulin resistance indexinsulin levels. Arhalofenate (100 mg/kg, p.o.) obviously increases the glucose infusion rate and decreases hepatic glucose output in the clamped state in Zucker Diabetic Fatty (ZDF) rats. Arhalofenate (100 mg/kg, p.o.) significantly reduces triglyceride, free fatty acid, and cholesterol levels in ZDF rats. Arhalofenate (100 mg/kg, p.o.) also significantly lowers fasting plasma insulin, and robustly decreases fasting plasma triglycerides after 32 days of treatment in Zucker Fatty (ZF) rats.
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• In Vitro:
  Arhalofenate displays a dose-dependent activation of mouse GAL4-PPAR-γ (EC50s: appr 12 μM). Arhalofenate is a prodrug ester, that is rapidly and completely modified in vivo by non-specific serum esterases to the mature free acid form Arhalofenate (MBX 102) acid. .
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Storage & Handling

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

Alternative Names

Arhalofenate, inhibit, JNJ39659100, JNJ-39659100, JNJ 39659100, Inhibitor, MBX 102, MBX102, MBX-102, PPAR-γ, PPARγ, PPAR, Peroxisome proliferator-activated receptors

Compound Identifiers

PubChem CID

12082259