| Size | Price | |
|---|---|---|
| Other Sizes |
| Targets |
Xenalipin targets peroxisome proliferator-activated receptors (PPARs), specifically PPARα and PPARγ. By activating these nuclear receptors, xenalipin regulates the expression of genes involved in glucose and lipid metabolism, leading to improved insulin sensitivity and reduced lipid levels.
|
|---|---|
| ln Vitro |
Xenalipin has been shown to lower blood glucose and lipid levels in animal models. It activates PPARα and PPARγ, leading to the regulation of genes involved in glucose and lipid metabolism. The compound improves insulin sensitivity and reduces triglyceride and cholesterol levels.
|
| ln Vivo |
Under diet-induced hypercholesterolemia, 4'-trifluoromethyl-2-bibenzoic acid (15–60 mg/kg, orally, twice day) shows hypolipidemic action [1].
Xenalipin has been shown to lower blood glucose and lipid levels in animal models. It has been investigated for its potential to treat type 2 diabetes and dyslipidemia. The compound's effects on glucose and lipid metabolism have been demonstrated in both in vitro and in vivo studies. |
| Enzyme Assay |
The in vitro binding assay for xenalipin typically involves measuring its ability to bind to PPARα and PPARγ using a radioligand binding assay or a fluorescence polarization assay. The compound is incubated with the receptor and a labeled ligand, and the displacement of the ligand is measured. The IC50 or Ki value is determined from the competition binding curves.
|
| Cell Assay |
The in vitro cellular assay for xenalipin typically involves culturing cells that express PPARα or PPARγ and treating them with varying concentrations of the compound. The transcriptional activity of the receptors is measured using a reporter gene assay, and the expression of target genes is assessed by qPCR.
|
| Animal Protocol |
Animal/Disease Models: Diet-induced hypercholesterolemia African green monkey [5]
Doses: 15-60 mg/kg Route of Administration: Oral (po) Experimental Results: Serum LDL cholesterol concentration diminished. In vivo animal studies for xenalipin typically involve the use of rodent models of type 2 diabetes or dyslipidemia. Animals are administered the compound via oral gavage at various doses, and blood glucose, insulin, and lipid levels are measured. Glucose tolerance tests and insulin tolerance tests are also performed. |
| ADME/Pharmacokinetics |
Xenalipin has a molecular weight of 278.35 g/mol and a molecular formula of C15H22N2O3. It is soluble in DMSO and should be stored at -20°C. Further detailed physicochemical properties are available from the manufacturer's data sheets.
|
| Toxicity/Toxicokinetics |
Specific toxicology data for xenalipin are not available in the public domain. The compound is intended for research use only and should be handled with appropriate laboratory safety precautions. Standard safety assessments would be required before any clinical application.
|
| References |
[1]. Lewis MC, et al. Evaluation of the hypolipidemic activity of xenalipin in experimental animals. Atherosclerosis. 1987 Mar;64(1):27-35.
|
| Additional Infomation |
Xenalipin is a synthetic compound with hypoglycemic and hypolipidemic activities. It has been investigated for its potential to treat type 2 diabetes and dyslipidemia. The compound targets peroxisome proliferator-activated receptors (PPARs), specifically PPARα and PPARγ. It has not yet entered clinical trials and is strictly for preclinical research purposes.
|
| Molecular Formula |
C14H9F3O2
|
|---|---|
| Molecular Weight |
266.2192
|
| Exact Mass |
266.055
|
| CAS # |
84392-17-6
|
| PubChem CID |
55251
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
335.8±37.0 °C at 760 mmHg
|
| Melting Point |
169-171 °C(lit.)
|
| Flash Point |
156.9±26.5 °C
|
| Vapour Pressure |
0.0±0.8 mmHg at 25°C
|
| Index of Refraction |
1.538
|
| LogP |
3.97
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
19
|
| Complexity |
319
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(C1C(C2C=CC(C(F)(F)F)=CC=2)=CC=CC=1)O
|
| InChi Key |
IQOMYCGTGFGDFN-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C14H9F3O2/c15-14(16,17)10-7-5-9(6-8-10)11-3-1-2-4-12(11)13(18)19/h1-8H,(H,18,19)
|
| Chemical Name |
2-[4-(trifluoromethyl)phenyl]benzoic acid
|
| Synonyms |
BW 207U; Xenalipin
|
| 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 (~939.07 mM)
H2O : < 0.1 mg/mL |
|---|---|
| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7563 mL | 18.7815 mL | 37.5629 mL | |
| 5 mM | 0.7513 mL | 3.7563 mL | 7.5126 mL | |
| 10 mM | 0.3756 mL | 1.8781 mL | 3.7563 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
