Inolitazone

SKU: orb1308191

Description

Inolitazone

Research Area

Metabolism Research, Molecular Biology

Key Properties

• CAS Number: 223132-37-4
• MW: 502.58
• Purity: 99.58% (May vary between batches)
• Formula: C₂₇H₂₆N₄O₄S
• SMILES: CN1C=2C(N=C1COC3=CC=C(CC4C(=O)NC(=O)S4)C=C3)=CC=C(OC5=CC(C)=C(N)C(C)=C5)C2
• Target: PPAR
• Solubility: DMSO:55 mg/mL (109.44 mM)

Bioactivity

• In Vivo:
  In athymic nude mice prior to DRO tumor cell implantation, Inolitazone inhibits tumor growth in a dose responsive fashion. 0.025% Inolitazone inhibits growth on day 32 by 94.4%. In the 0.0025% treatment group, tumor growth is inhibited by 62.3% while the 0.00025% dose demonstrated no growth inhibitory activity as compared to control. Inolitazone treated animals demonstrate tumor growth inhibition of 68.9% in DRO tumors and 48.3% in ARO tumors on day 35. Inolitazone plus Paclitaxel demonstrate additive antiproliferative activity in cell culture and minimal ATC tumor growth.
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• In Vitro:
  Inolitazone (10 nM) inhibits the growth of DRO cells through a PPARγ-dependent mechanism. Inolitazone upregulates the cell cycle kinase inhibitor, p21WAF1/CIP1. Inolitazone (10 nM) activates PPARγ:RXRα-dependent transcription utilizing a PPRE response element fused to a luciferase reporter gene (PPRE3-tk-luc). Inolitazone specifically activates PPARγ, but not PPARα or PPARδ. Inolitazone (10 nM) following transient transfection with the appropriate PPAR isoform (γ, α, or δ) and PPAR response element linked to a luciferase reporter in RIE rat small intestinal cell line, which does not express PPARs, yields increased luciferase activity only in the presence of PPARγ and PPRE3-tk-luc.
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Storage & Handling

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

Alternative Names

RS 5444, RS5444, RS-5444, PPAR, PPARγ, Peroxisome proliferator-activated receptors, inhibit, Efatutazone, Inolitazone, Inhibitor, CS7017, CS-7017, CS 7017

Compound Identifiers

PubChem CID

9832447