| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
The primary targets of Netoglitazone are PPAR-α and PPAR-γ, which are nuclear receptors involved in glucose and lipid metabolism. Activation of PPAR-γ increases insulin sensitivity in adipose tissue, muscle, and liver, while PPAR-α activation promotes fatty acid oxidation. Netoglitazone is a full agonist of PPAR-γ and a partial agonist of PPAR-α, giving it a unique profile.
|
|---|---|
| ln Vitro |
In vitro, Netoglitazone demonstrates potent agonist activity at PPAR-γ with an EC₅₀ in the nanomolar range. It also activates PPAR-α with a lower potency. In cell-based reporter assays, it induces the expression of PPAR target genes involved in glucose uptake and lipid storage. It also inhibits adipocyte differentiation. These effects are concentration-dependent.
|
| ln Vivo |
In vivo, Netoglitazone has shown glucose-lowering effects in diabetic animal models, such as ob/ob mice and Zucker diabetic fatty rats. It reduces insulin resistance and lowers circulating free fatty acids. However, it has been associated with fluid retention and weight gain, which are common side effects of TZDs. Its development was halted due to hepatotoxicity in some studies.
|
| Enzyme Assay |
In vitro receptor binding assays for Netoglitazone measure its affinity for PPAR-α and PPAR-γ using radioligand competition or time-resolved fluorescence resonance energy transfer (TR-FRET). The compound's ability to recruit coactivators is assessed in cell-based transactivation assays. IC₅₀ or EC₅₀ values are determined.
|
| Cell Assay |
In vitro cell-based assays for Netoglitazone evaluate its effects on glucose uptake and adipogenesis. 3T3-L1 preadipocytes are treated with the compound, and differentiation is assessed by Oil Red O staining. Glucose uptake is measured using 2-deoxyglucose uptake assays in muscle or adipocyte cells. Gene expression of PPAR targets is measured by qRT-PCR.
|
| Animal Protocol |
In vivo animal studies for Netoglitazone involve diabetic rodent models. The compound is administered orally, and blood glucose and insulin levels are monitored. Oral glucose tolerance tests (OGTT) are performed. Body weight and food intake are recorded. Tissue biopsies are analyzed for PPAR target gene expression.
|
| ADME/Pharmacokinetics |
The pharmacokinetic properties of Netoglitazone include good oral bioavailability and a long half-life. It is highly protein-bound. The compound is metabolized by CYP3A4. Its molecular weight is 397.49 g/mol. Storage is at -20°C.
|
| Toxicity/Toxicokinetics |
The toxicity profile of Netoglitazone includes hepatotoxicity, as well as fluid retention and weight gain. It has been associated with bladder cancer risk in some studies, though this is debated. Due to these concerns, it was not approved for clinical use.
|
| References | |
| Additional Infomation |
Neiglitazone (MCC-555) is a hypoglycemic drug. It belongs to the thiazide class of antidiabetic drugs and has hypoglycemic activity. Neiglitazone also possesses peroxisome proliferator-activated receptor (PPAR) α and γ agonist activity. In vivo, neiglitazone can reduce bone formation and increase bone marrow adipocyte formation.
Additional information: Netoglitazone is also known as MCC-555. It is a PPAR dual agonist. It is a research compound for studying PPAR biology and diabetes. This product is for research use only and is not approved for clinical or therapeutic applications. |
| Molecular Formula |
C21H16NO3FS
|
|---|---|
| Molecular Weight |
381.42004
|
| Exact Mass |
381.083
|
| CAS # |
161600-01-7
|
| PubChem CID |
204109
|
| Appearance |
White to yellow solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
599.5±30.0 °C at 760 mmHg
|
| Flash Point |
316.4±24.6 °C
|
| Vapour Pressure |
0.0±1.7 mmHg at 25°C
|
| Index of Refraction |
1.668
|
| LogP |
4.5
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
27
|
| Complexity |
560
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
PKWDZWYVIHVNKS-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C21H16FNO3S/c22-18-4-2-1-3-16(18)12-26-17-8-7-14-9-13(5-6-15(14)11-17)10-19-20(24)23-21(25)27-19/h1-9,11,19H,10,12H2,(H,23,24,25)
|
| Chemical Name |
5-[[6-[(2-fluorophenyl)methoxy]naphthalen-2-yl]methyl]-1,3-thiazolidine-2,4-dione
|
| HS Tariff Code |
2934.99.9001
|
| 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 Vitro) |
DMSO : ~250 mg/mL (~655.45 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.45 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 20.8 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: 2.08 mg/mL (5.45 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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: ≥ 2.08 mg/mL (5.45 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 | 2.6218 mL | 13.1089 mL | 26.2178 mL | |
| 5 mM | 0.5244 mL | 2.6218 mL | 5.2436 mL | |
| 10 mM | 0.2622 mL | 1.3109 mL | 2.6218 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
