Name: LXR-623
Price: 214.00 USD

- Overview
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    Background
    
    LXR-623 is an agonist of liver X-receptor with IC50 values of 179nM and 24nM for LXR-α and LXR-β, respectively [1].
    LXR-623 is a partial agonist of LXR which regulates the transcription of genes involved in cellular cholesterol homeostasis. As the LXR agonist, LXR-623 is used to enhance reverse cholesterol transport through up-regulating cholesterol transporters. To rodents, orally dosed LXR-623 increases the transcription level of ABCA1 and ABCG1 in peripheral blood cells. To human, LXR-623 also significantly increases ABCA1 and ABCG1 both in PBMC cells and in T- and B-cells. In addition, in mouse model of atherosclerosis, LXR-623 is found to up-regulate intestinal ABCG5 and ABCG8. In cynomolgus monkeys, LXR-623 up-regulates ABCA1 and ABCG1 in whole blood. Besides that, LXR-623 is proposed to be used in treatment of Alzheimer’s disease since it can lower the level of amyloid-βin brain [1, 2].
    
    [1] Katz A, Udata C, Ott E, et al. Safety, Pharmacokinetics, and Pharmacodynamics of Single Doses of LXR‐623, a Novel Liver X‐Receptor Agonist, in Healthy Participants. The Journal of Clinical Pharmacology, 2009, 49(6): 643-649.
    [2] DiBlasio-Smith E A, Arai M, Quinet E M, et al. Discovery and implementation of transcriptional biomarkers of synthetic LXR agonists in peripheral blood cells. J Transl Med, 2008, 6: 59.
- Properties
  - Categories
    
    Liver X-receptor agonist
    
    Alternative Name
    
    2-[(2-chloro-4-fluorophenyl)methyl]-3-(4-fluorophenyl)-7-(trifluoromethyl)indazole
    
    CAS Number
    
    875787-07-8
    
    Molecular Formula
    
    C21H12ClF5N2
    
    Molecular Weight
    
    422.78
    
    Appearance
    
    A solid
    
    Purity
    
    99.76%
    
    Solubility
    
    insoluble in H2O; ≥15.49 mg/mL in EtOH with ultrasonic; ≥19.4 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    C1=CC2=C(N(N=C2C(=C1)C(F)(F)F)CC3=C(C=C(C=C3)F)Cl)C4=CC=C(C=C4)F
    
    * For Research Use Only
- Reference
  - 1. Xu D, He H, et al. "SIRT2 plays a novel role on progesterone, estradiol and testosterone synthesis via PPARs/LXRα pathways in bovine ovarian granular cells." J Steroid Biochem Mol Biol. 2018 Aug 7. pii: S0960-0760(18)30023-2. PMID:30009951
    2. Xian X, Ding Y, et al. "LRP1 integrates murine macrophage cholesterol homeostasis and inflammatory responses in atherosclerosis."Elife. 2017 Nov 16;6. pii: e29292. PMID:29144234