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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- CAS No.: 331248-11-4
- 화학식: C25H34F2O3
- 분자량:420.53
-
보관:
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]
-
Biological Activity
-
Chemical Information
- 순도&문서
- References
-
Help & FAQs
Biological Activity
Ki: 2.7 nM (RXRα)[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CV-1 | EC50 |
11 nM
Compound: LG0101506
|
Transcriptional activation in CV-1 cells expressing Retinoic X receptor alpha
Transcriptional activation in CV-1 cells expressing Retinoic X receptor alpha
|
[PMID: 15006411] |
| 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] |
| CV-1 | EC50 |
3.1 nM
Compound: 1
|
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
|
[PMID: 12951091] |
| CV-1 | IC50 |
8 nM
Compound: 4
|
In vitro transcriptional activation in CV-1 cells expressing RXR-alpha
In vitro transcriptional activation in CV-1 cells expressing RXR-alpha
|
[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.
-
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.
-
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.
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).
Chemical Information
-
CAS No. 331248-11-4
-
분자량 420.53
-
화학식 C25H34F2O3
-
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
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[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
Powered by Bioz