| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| ln Vitro |
Inolitazone diHClide (Efatutazone diHClide) increases the expression of p21WAF1/CIP1, a cell cycle kinase inhibitor. Cells that have p21WAF1/CIP1 silenced become resistant to inolitazone. Using a PPRE response element coupled to a luciferase reporter (PPRE3-tk-luc), a transient transfection test shows that inolitazone at a concentration of 10 nM activates PPARγ:RXRα-dependent transcription. The appropriate concentrations of Inolitazone, Rosiglitazone, or Troglitazone were applied to DRO cells in culture. PPRE3-tk-luc was transiently transfected into DRO cells in order to measure the effective concentration at which EC50 is reached. Inolitazone's EC50 is 1 nM, rosiglitazone's is 65 nM, and troglitazone's is 631 nM. Likewise, 0.8 nM for Inolitazone, 75 nM for Rosiglitazone, and 1412 nM for Troglitazone were determined to have the IC50 inhibitory values. PPARγ is selectively activated by inolitazone, but PPARα and PPARδ are not. After transient transfection with the relevant PPAR isoform (γ, α, or δ) and a PPAR response element connected to a luciferase reporter gene, a 10 nM Inolitazone alone was applied in the presence of PPARγ and PPRE3-tk-luc in a RIE rat intestinal cell line that does not express PPAR [1]. DRO cell proliferation is inhibited by 10 nM Inolitazone (RS5444) via a PPARγ-dependent mechanism [2].
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| ln Vivo |
Paclitaxel plus inolitazone diHCl (Efatutazone diHClide) reduces the growth of ATC tumors and shows further antiproliferative effect in cell culture. Tumor growth was dose-responsively decreased when athymic nude mice receiving inolitazone via the diet before DRO tumor cell implantation. On day 32, the maximum dosage of 0.025% Inolitazone reduced growth by 94.4% in comparison to the control. Five out of ten rats in this therapy group did not have visible tumors. Tumor growth was suppressed by 62.3% in the 0.0025% treatment group on day 32 when compared to the control, but no growth inhibitory effect was observed in the 0.00025% dosage group. After a week of DRO or ARO tumor cell implantation, mice bearing tumors were given 0.025% Inolitazone treatment. Tumors were permitted to form nests in the mice. When compared to their respective controls, mice treated with Inolitazone on day 35 showed 68.9% tumor growth inhibition in DRO tumors and 48.3% tumor growth inhibition in ARO tumors [1].
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| References |
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| Additional Infomation |
Efatutazone Dihydrochloride is the dihydrochloride salt of efatutazone, an orally bioavailable agonist of peroxisome proliferator-activated receptor gamma (PPAR-gamma) with potential antineoplastic activity. Efatutazone binds to and activates PPAR-gamma, a nuclear hormone receptor and a ligand-activated transcription factor controling gene expression involved in macromolecule metabolism and cell differentiation, specifically adipocyte differentiation. Mediated through activation of PPAR-gamma, this agent is capable of inducing cell differentiation and apoptosis, thereby leading to a reduction in cellular proliferation.
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| Molecular Formula |
C27H28CL2N4O4S
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|---|---|
| Molecular Weight |
575.51
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| Exact Mass |
574.121
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| CAS # |
223132-38-5
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| Related CAS # |
Inolitazone;223132-37-4
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| PubChem CID |
16719220
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| Appearance |
Pale purple to purple solid powder
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| LogP |
7.498
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
38
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| Complexity |
782
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WFIOHOJEIMQCEG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H26N4O4S.2ClH/c1-15-10-20(11-16(2)25(15)28)35-19-8-9-21-22(13-19)31(3)24(29-21)14-34-18-6-4-17(5-7-18)12-23-26(32)30-27(33)36-23;;/h4-11,13,23H,12,14,28H2,1-3H3,(H,30,32,33);2*1H
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| Chemical Name |
5-[[4-[[6-(4-amino-3,5-dimethylphenoxy)-1-methylbenzimidazol-2-yl]methoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione;dihydrochloride
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| Synonyms |
CS-7017 CS 7017 Efatutazone hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~43.44 mM)
H2O : ~1 mg/mL (~1.74 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.34 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7376 mL | 8.6879 mL | 17.3759 mL | |
| 5 mM | 0.3475 mL | 1.7376 mL | 3.4752 mL | |
| 10 mM | 0.1738 mL | 0.8688 mL | 1.7376 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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