2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. RAR/RXR
  4. 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.

For research use only. We do not sell to patients.

LG101506 Chemical Structure

LG101506 Chemical Structure

CAS No. : 331248-11-4

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LG101506 Related Antibodies

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Description

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[1][2].

IC50 & Target

Ki: 2.7 nM (RXRα)[1]
Cellular Effect
Cell Line Type Value Description References
CV-1 EC50
131.5 nM
Compound: 4
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
[PMID: 12954061]
In Vitro

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.

LG101506 Related Antibodies

Western Blot Analysis[2]

Cell Line: RAW264.7 cells
Concentration: 100, 300 and 1000 nM
Incubation Time: 24 h
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.

Western Blot Analysis[2]

Cell Line: U937 leukemia cells
Concentration: 30 and 100 nM
Incubation Time: 1, 2, 8 and 24 h
Result: Enhanced phosphorylation of Akt in U937 cells within 1 hour, which increased further at 8 hours.
In Vivo

LG101506 (10 mg/kg; in diet for 16 weeks) suppresses lung carcinogenesis in A/J mice[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: A/J mice, lung carcinogenesis model[2]
Dosage: 40 mg/kg diet or approximately 10 mg/kg body weight
Administration: Oral, for 16 weeks
Result: Reduced the number of lung tumors, the average tumor burden, the size and histopathology of lung tumors.
Animal Model: Male ICR mice[1]
Dosage: 30 mg/kg
Administration: Oral (Pharmacokinetic Analysis)
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).
Molecular Weight

420.53

Formula

C25H34F2O3
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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LG101506 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LG101506331248-11-4LG 101506LG-101506RAR/RXRRetinoic acid receptorsRetinoid X receptorsanti-inflammatorycancertype 2 diabetesRAW264.7TNFαInhibitorinhibitorinhibit

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