CAS 153559-76-3|LG100268
| Common Name | LG100268 | ||
|---|---|---|---|
| CAS Number | 153559-76-3 | Molecular Weight | 363.49300 |
| Density | 1.115g/cm3 | Boiling Point | 487ºC at 760mmHg |
| Molecular Formula | C24H29NO2 | Melting Point | 275-277ºC |
| MSDS | USA | Flash Point | 248.3ºC |
Names
| Name | 6-[1-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)cyclopropyl]pyridine-3-carboxylic acid |
|---|---|
| Synonym | More Synonyms |
LG100268 BiologicalActivity
| 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 >>AutophagyResearch Areas >>Metabolic DiseaseSignaling 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 |
Toxicological Information
CHEMICAL IDENTIFICATION |
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 |
|---|
Articles5
More 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 (... |
Synonyms
| AmbkkkkK580 |
| BIDD:PXR0022 |
