Inolitazone free base
Inolitazone a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC50 of 0.8 nM for growth inhibition.
For research use only. Not for human or veterinary use.
Inolitazone structure
CAS No.: 223132-37-4
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 50 mg | USD 440.00 | BP-00022-50mg | In stock | Get quote |
| 100 mg | USD 700.00 | BP-00022-100mg | In stock | Get quote |
| 250 mg | USD 1,400.00 | BP-00022-250mg | In stock | Get quote |
| 500 mg | USD 2,250.00 | BP-00022-500mg | In stock | Get quote |
| 1 g | USD 3,600.00 | BP-00022-1g | In stock | Get quote |
| 2 g | Inquire | BP-00022-2g | In stock | Inquire |
| 3 g | Inquire | BP-00022-3g | In stock | Inquire |
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Description
Inolitazone a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC50 of 0.8 nM for growth inhibition.
Biological activity
In Vitro Inolitazone (RS5444) upregulates the cell cycle kinase inhibitor, p21 WAF1/CIP1. Silencing p21 WAF1/CIP1 rendered cells insensitive to Inolitazone. A 10 nM dose of Inolitazone activates PPARγ:RXRα-dependent transcription as demonstrated in a transient transfection assay utilizing a PPRE response element fused to a luciferase reporter gene (PPRE3-tk-luc). DRO cells are treated in culture with Inolitazone, Rosiglitazone, or Troglitazone at the indicated concentrations. DRO cells are transiently transfected with PPRE3-tk-luc to examine effective concentrations at which EC50 occurs. The EC50s are 1 nM (Inolitazone), 65 nM (Rosiglitazone) and 631 nM (Troglitazone). Similarly, the calculated inhibitory concentration at IC50 is 0.8 nM for Inolitazone, 75 nM for Rosiglitazone, and 1412 nM for Troglitazone. Inolitazone specifically activates PPARγ, but not PPARα or PPARδ. Exposure of 10 nM Inolitazone 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[1]. DRO cells are growth inhibited by 10 nM Inolitazone (RS5444) through a PPARγ-dependent mechanism. In Vivo Inolitazone (RS5444) plus Paclitaxel demonstrate additive antiproliferative activity in cell culture and minimal ATC tumor growth. When Inolitazone is administered in the diet to athymic nude mice prior to DRO tumor cell implantation, tumor growth is inhibited in a dose responsive fashion. At the highest dose, 0.025% Inolitazone inhibits growth on day 32 by 94.4% as compared to that of control. In this treatment group, five of 10 animals do not develop demonstrable tumors. In the 0.0025% treatment group, tumor growth is inhibited by 62.3% compared to that of control on day 32 while the 0.00025% dose demonstrated no growth inhibitory activity as compared to control. Tumors is nest allowed to establish in the mouse and began 0.025% Inolitazone treatment of mice 1 week after DRO or ARO tumor cell implantation. Inolitazone treated animals demonstrate tumor growth inhibition of 68.9% in DRO tumors and 48.3% in ARO tumors as compared to that of their respective controls on day 35.
Identifiers
- SMILES
-
O=C1SC(C(=O)N1)CC2=CC=C(OCC3=NC=4C=CC(OC=5C=C(C(N)=C(C5)C)C)=CC4N3C)C=C2 - InChIKey
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JCYNMRJCUYVDBC-UHFFFAOYSA-N
Specifications
- MW (average)
- 502.5850
- Formula
- C27H26N4O4S
- CAS No.
- 223132-37-4
- Physical state
- Solid
- Color
- White to off-white
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Please store the product under the recommended conditions in the Certificate of Analysis.