| Size | Price | |
|---|---|---|
| 10mg | ||
| 25mg | ||
| 50mg | ||
| 100mg | ||
| 250mg |
Purity: ≥98%
Description: Imiglitazar (also known as TAK559; proposed tradename Pargluva) is a novel, potent and dual human peroxisome proliferator-activated receptor PPARα and PPARγ1 agonist with EC50 values of 67 and 31 nM and with hypoglycemic activity. Muraglitazar had completed phase III clinical trials, however in May, 2006 Bristol-Myers Squibb announced that it had discontinued further development.. Data on muraglitazar isrelatively sparse due to the recent introduction of this agent.
| ln Vitro |
Approximately 68% of the maximal activation of rosiglitazone, a recognized PPARγ agonist, is exhibited by TAK-559, a partial agonist of hPPARg1. When TAK-559 is present at high doses (10 μM), PPARγ is markedly activated. TAK-559 directly binds to each hPPAR isoform, transactivating all of the isoforms, as shown by competition binding experiments with radiolabeled ligands. Additionally, TAK-559 dissociates the corepressor NCoR from hPPARγ1 and hPPARα and recruits the coactivator SRC-1 to hPPARγ1 and hPPARα [1]. In the presence of 10 μM TAK-559, TNFα or IL-1β-induced THP-1 cell adhesion to cultivated endothelium cells was dramatically inhibited. When 10 μM TAK-559 was present, endothelial cells secreted 36% less monocyte chemoattractant protein-1 (MCP-1), which was followed by a decrease in intracellular mRNA expression. TAK-559 dramatically inhibits the migration and proliferation of cultured smooth muscle cells [2].
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| ln Vivo |
High-density lipoprotein (HDL) cholesterol levels significantly increased after receiving TAK-559 treatment; this rise was accompanied by a decrease in tiny dense HDL particles and an increase in large HDL particles. Apolipoprotein AI levels rose and plasma triglyceride and apolipoprotein B-100 levels fell during TAK-559 treatment. The highest dose of 3.0 mg/kg per day was shown to significantly address insulin resistance and hyperinsulinemia in these prediabetic monkeys. Moreover, during the study period, no negative effects were noted on typical liver function measures [3].
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| References |
[1]. Sakamoto J, et al. A novel oxyiminoalkanoic acid derivative, TAK-559, activates human peroxisome proliferator-activated receptor subtypes. Eur J Pharmacol. 2004 Jul 8;495(1):17-26.
[2]. Seki N, et al. A potent activator of PPARalpha and gamma reduces the vascular cell recruitment and inhibits the intimal thickning in hypercholesterolemic rabbits. Atherosclerosis. 2005 Jan;178(1):1-7. [3]. Ding SY, et al. A novel peroxisome proliferator--activated receptor alpha/gamma dual agonist ameliorates dyslipidemia and insulin resistance in prediabetic rhesus monkeys. Metabolism. 2007 Oct;56(10):1334-9 |
| Molecular Formula |
C28H26N2O5
|
|---|---|
| Molecular Weight |
470.516447544098
|
| CAS # |
250601-04-8
|
| SMILES |
O=C(O)CC/C(C1=CC=CC=C1)=N\OCC2=CC=C(OCC3=C(C)OC(C4=CC=CC=C4)=N3)C=C2
|
| InChi Key |
ULVDFHLHKNJICZ-QCWLDUFUSA-N
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| InChi Code |
InChI=1S/C28H26N2O5/c1-20-26(29-28(35-20)23-10-6-3-7-11-23)19-33-24-14-12-21(13-15-24)18-34-30-25(16-17-27(31)32)22-8-4-2-5-9-22/h2-15H,16-19H2,1H3,(H,31,32)/b30-25+
|
| Chemical Name |
Benzenebutanoic acid, gamma-(((4-((5-methyl-2-phenyl-4-oxazolyl)methoxy)phenyl)methoxy)imino)-, (gammaE)-
|
| Synonyms |
TAK 559; TAK-559; TAK559.
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1253 mL | 10.6265 mL | 21.2531 mL | |
| 5 mM | 0.4251 mL | 2.1253 mL | 4.2506 mL | |
| 10 mM | 0.2125 mL | 1.0627 mL | 2.1253 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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