| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Ki: 2.7 nM (RXRα)[1]
|
|---|---|
| ln Vitro |
LG101506 and BRL 49653 work together to improve RXR/PPARγ heterodimer activation, with an EC50 of 3.1 nM [1]. In RAW264.7 cells, LPS-stimulated NO generation is blocked within 24 hours by LG101506 (15.6-1000 nM) in a dose-dependent manner [2]. In RAW264.7 cells, LPS or TNFα-induced inflammatory pathways are inhibited by LG101506 (100-1000 nM; 24 h) [2]. U937 leukemia cells are differentiated by LG101506 (30 and 100 nM; 1–24 h) [2].
|
| ln Vivo |
For 16 weeks, the A/J mice's diet containing 10 mg/kg of LG101506 prevents the development of lung cancer[2].
|
| Cell Assay |
Western Blot Analysis[2]
Cell Types: RAW264.7 cells Tested Concentrations: 100, 300 and 1000 nM Incubation Duration: 24 h Experimental Results: Markedly diminished protein levels of COX-2. Pretreatment prevented the degradation of IκBα in RAW cells stimulated with TNFα. Enhanced Erk phosphorylation, which peaked at 8 hrs (hours). Western Blot Analysis[2] Cell Types: U937 leukemia cells Tested Concentrations: 30 and 100 nM Incubation Duration: 1, 2, 8 and 24 h Experimental Results: Enhanced phosphorylation of Akt in U937 cells within 1 hour, which increased further at 8 hrs (hours). |
| Animal Protocol |
Animal/Disease Models: A/J mice, lung carcinogenesis model[2]
Doses: 40 mg/kg diet or approximately 10 mg/kg body weight Route of Administration: po (oral gavage) for 16 weeks Experimental Results: decreased the number of lung tumors, the average tumor burden, the size and histopathology of lung tumors. Animal/Disease Models: Male ICR mice[1] Doses: 30 mg/kg Route of Administration: Oral (pharmacokinetic/PK Analysis) Experimental Results: In vivo evaluation of oral exposure of LG101506[1] Compd Dose (mg/kg) Oral AUC(0-6 h) (μg·h/mL) Tmax (h) Cmax (μg·h/mL) LG101506 30 2.09±0.45 1 1.2±0.28 Data collected in male ICR mouse using a dose formulation of the free acid in CMC/SLS/Povidone (30 mg/kg). Timepoints: 1, 3, 8 h (serial sacrifice, n=3/time point). |
| References |
| Molecular Formula |
C25H34O3F2
|
|---|---|
| Molecular Weight |
420.53246
|
| Exact Mass |
420.248
|
| CAS # |
331248-11-4
|
| PubChem CID |
9845057
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
6.915
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
30
|
| Complexity |
663
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
FC(F)COC1C(C(C)(C)C)=CC(C(C)(C)C)=CC=1/C(/C)=C/C=C/C(/C)=C/C(O)=O
|
| InChi Key |
BHIBZAZKKARFIM-XRYBSMBUSA-N
|
| InChi Code |
InChI=1S/C25H34F2O3/c1-16(12-22(28)29)10-9-11-17(2)19-13-18(24(3,4)5)14-20(25(6,7)8)23(19)30-15-21(26)27/h9-14,21H,15H2,1-8H3,(H,28,29)/b10-9+,16-12+,17-11-
|
| Chemical Name |
(2E,4E,6Z)-7-[3,5-ditert-butyl-2-(2,2-difluoroethoxy)phenyl]-3-methylocta-2,4,6-trienoic acid
|
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 2.3780 mL | 11.8898 mL | 23.7795 mL | |
| 5 mM | 0.4756 mL | 2.3780 mL | 4.7559 mL | |
| 10 mM | 0.2378 mL | 1.1890 mL | 2.3780 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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