LG101506
LG101506 is a selective and orally active RXR modulator with a Ki of 2.7 nM for RXRα. LG101506 can be used for the research of type 2 diabetes and cancer.
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- CAS No.: 331248-11-4
- Formule: C25H34F2O3
- Masse moléculaire:420.53
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Ki: 2.7 nM (RXRα)[1]
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Cell Line
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Type | Value | Description | References |
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| CV-1 | EC50 |
11 nM
Compound: LG0101506
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Transcriptional activation in CV-1 cells expressing Retinoic X receptor alpha
Transcriptional activation in CV-1 cells expressing Retinoic X receptor alpha
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[PMID: 15006411] |
| CV-1 | EC50 |
131.5 nM
Compound: 4
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In vitro evaluation against RXR-alpha/PPAR-gamma in CV-1 cells by cotransfection assay was determined
In vitro evaluation against RXR-alpha/PPAR-gamma in CV-1 cells by cotransfection assay was determined
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[PMID: 12954061] |
| CV-1 | EC50 |
3.1 nM
Compound: 1
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Synergistic activation of BRL-49653 mediated PPAR gamma and retinoid X receptor alpha expressed in CV-1 cell transcriptional activation assay
Synergistic activation of BRL-49653 mediated PPAR gamma and retinoid X receptor alpha expressed in CV-1 cell transcriptional activation assay
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[PMID: 12951091] |
| CV-1 | IC50 |
8 nM
Compound: 4
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In vitro transcriptional activation in CV-1 cells expressing RXR-alpha
In vitro transcriptional activation in CV-1 cells expressing RXR-alpha
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[PMID: 12954061] |
LG101506 synergizes with BRL 49653 (HY-17386) to enhance activation at the RXR/PPARγ heterodimer with an EC50 of 3.1 nM[1].
LG101506 (15.6-1000 nM) blocks the production of NO in a dose-dependent manner in RAW264.7 stimulated with LPS (HY-D1056) for 24 hours[2].
LG101506 (100-1000 nM; 24 h) inhibits inflammatory pathways induced by LPS (HY-D1056) or TNFα in RAW264.7 cells[2].
LG101506 (30 and 100 nM; 1-24 h) induces differentiation in U937 leukemia cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW264.7 cells
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Concentration:100, 300 and 1000 nM
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Incubation Time:24 h
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Result:Markedly reduced protein levels of COX-2. Pretreatment prevented the degradation of IκBα in RAW cells stimulated with TNFα. Enhanced Erk phosphorylation, which peaked at 8 hours.
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Cell Line:U937 leukemia cells
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Concentration:30 and 100 nM
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Incubation Time:1, 2, 8 and 24 h
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Result:Enhanced phosphorylation of Akt in U937 cells within 1 hour, which increased further at 8 hours.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A/J mice, lung carcinogenesis model[2]
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Dosage:40 mg/kg diet or approximately 10 mg/kg body weight
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Administration:Oral, for 16 weeks
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Result:Reduced the number of lung tumors, the average tumor burden, the size and histopathology of lung tumors.
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Animal Model:Male ICR mice[1]
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Dosage:30 mg/kg
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Administration:Oral (Pharmacokinetic Analysis)
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Result: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).
Chemical Information
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CAS No. 331248-11-4
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Masse moléculaire 420.53
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Formule C25H34F2O3
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SMILES
FC(F)COC1=C(C=C(C=C1/C(C)=C\C=C\C(C)=C\C(O)=O)C(C)(C)C)C(C)(C)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Gernert DL, et al. Design and synthesis of fluorinated RXR modulators. Bioorg Med Chem Lett. 2003 Oct 6;13(19):3191-5. [Content Brief]
[2]. Cao M, et al. The Rexinoids LG100268 and LG101506 Inhibit Inflammation and Suppress Lung Carcinogenesis in A/J Mice. Cancer Prev Res (Phila). 2016 Jan;9(1):105-14. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LG101506 Related Classifications
HY-108524 Related Classifications
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