1. Metabolic Enzyme/Protease
    Autophagy
  2. RAR/RXR
    Autophagy
  3. LG100268

LG100268 (Synonyms: LG268)

Cat. No.: HY-15340 Purity: 99.22%
Handling Instructions

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. 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. LG100268 activates RXR homodimers to induce transcriptional activation. LG100268 can be used for the study of lung carcinogenesisy.

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

LG100268 Chemical Structure

LG100268 Chemical Structure

CAS No. : 153559-76-3

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Based on 1 publication(s) in Google Scholar

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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].

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.
Molecular Weight

363.49

Formula

C₂₄H₂₉NO₂

CAS No.

153559-76-3

SMILES

O=C(C1=CC=C(C2(C3=C(C)C=C4C(C)(C)CCC(C)(C)C4=C3)CC2)N=C1)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 4.17 mg/mL (11.47 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7511 mL 13.7555 mL 27.5111 mL
5 mM 0.5502 mL 2.7511 mL 5.5022 mL
10 mM 0.2751 mL 1.3756 mL 2.7511 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.25 mg/mL (3.44 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.25 mg/mL (3.44 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.25 mg/mL (3.44 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

LG100268LG268LG 100268LG-100268LG 268LG-268RAR/RXRAutophagyRetinoic acid receptorsRetinoid X receptorsA/J miceRAW264.7,?breastlungcancerHypertriglyceridemiaInhibitorinhibitorinhibit

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LG100268
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HY-15340
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