LG100268

Names

[ Name ]:
LG100268

[Synonym ]:
AmbkkkkK580
BIDD:PXR0022

Biological Activity

[Description]:

LG100268 (LG268) is a potent, selective and orally active retinoid X receptor (RXR) agonist with EC50 values of 4 nM, 3 nM, and 4 nM for RXR-α, RXR-β, and RXR-γ, respectively[1]. LG100268 displays >1000-fold selectivity for RXR over RAR, the Ki values are 3.4 nM, 6.2 nM and 9.2 nM for RXR-α, RXR-β, and RXR-γ, respectively[2]. LG100268 activates RXR homodimers to induce transcriptional activation. LG100268 can be used for the study of lung carcinogenesisy[3].

[Related Catalog]:

Signaling Pathways >> Autophagy >> Autophagy

Research Areas >> Metabolic Disease

Signaling Pathways >> Metabolic Enzyme/Protease >> RAR/RXR

[In Vitro]

LG100268 (100 nM-1 μM; 24 hours) shows a downregulation of CSF3 and a 2.5-fold decrease of CXCL2 and IL-1β mRNA expression in RAW264.7 cells[3]. Cell Viability Assay[3] Cell Line: RAW264.7 cells Concentration: 100 nM-1 μM Incubation Time: 24 hours Result: Decreased LPS induced cytokine mRNA levels.

[In Vivo]

LG100268 (oral diet; 100 mg/kg; once daily; 7 weeks) combines with C/P presents a more markedly reduced average tumor burden than LG268 or C/P alone. The combination establish a reduced lung tumors, which represents a reduction of 82% (vs. 59%-67% with the single drugs) in comparison with the controls[3]. Animal Model: A/J mice[3] Dosage: 50 mg/kg (Combines with carboplatin (50 mg/kg i.p.) starts 1 week after the LG268 treatment diet) Administration: Oral diet; once daily; 7 weeks Result: Decreased lung tumors growth significantly in mice.

[References]

[1]. M F Boehm, et al. Design and Synthesis of Potent Retinoid X Receptor Selective Ligands That Induce Apoptosis in Leukemia Cells. J Med Chem

[2]. D S Lala, et al. Activation of Specific RXR Heterodimers by an Antagonist of RXR Homodimers.Nature. 1996 Oct 3;383(6599):450-3.

[3]. Martine Cao,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.

Chemical & Physical Properties

[ Density]:
1.115g/cm3

[ Boiling Point ]:
487ºC at 760mmHg

[ Melting Point ]:
275-277ºC

[ Molecular Formula ]:
C₂₄H₂₉NO₂

[ Molecular Weight ]:
363.49300

[ Flash Point ]:
248.3ºC

[ Exact Mass ]:
363.22000

[ PSA ]:
50.19000

[ LogP ]:
5.51710

[ Vapour Pressure ]:
0mmHg at 25°C

[ Index of Refraction ]:
1.577

[ Storage condition ]:
-20°C

MSDS

Click to get detail MSDS

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: US5921500

CHEMICAL NAME :: 3-Pyridinecarboxylic acid, 6-(1-(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naph thalenyl) cyclopropyl)-

CAS REGISTRY NUMBER :: 153559-76-3

LAST UPDATED :: 199806

DATA ITEMS CITED :: 1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 21780 ug/kg/3D-I

TOXIC EFFECTS :: Liver - other changes Biochemical - Effect on specific coenzyme - CoA

REFERENCE :: FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 33,264,1996

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Articles

The active enhancer network operated by liganded RXR supports angiogenic activity in macrophages.

Genes Dev. 28(14) , 1562-77, (2014)

RXR signaling is predicted to have a major impact in macrophages, but neither the biological consequence nor the genomic basis of its ligand activation is known. Comprehensive genome-wide studies were...

Tributyltin engages multiple nuclear receptor pathways and suppresses osteogenesis in bone marrow multipotent stromal cells.

Chem. Res. Toxicol. 28 , 1156-66, (2015)

Organotins are members of the environmental obesogen class of contaminants because they activate peroxisome proliferator-activated receptor γ (PPARγ), the essential regulator of adipogenesis. Exposure...

Research resource: transcriptome profiling of genes regulated by RXR and its permissive and nonpermissive partners in differentiating monocyte-derived dendritic cells.

Mol. Endocrinol. 24 , 2218-2231, (2010)

Retinoid X receptors (RXRs) are heterodimerization partners for many nuclear receptors and also act as homodimers. Heterodimers formed by RXR and a nonpermissive partner, e.g. retinoic acid receptor (...

Related Compounds

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