TLX activator-1
TLX activator-1 is a highly selective TLX activator with an EC50 of 0.010 μM. TLX activator-1 regulates gene expression, upregulates genes related to ATP production and lysosomal function, and inhibits genes associated with inflammatory signaling pathways and Apoptotic signaling pathways. TLX activator-1 exhibits anti-neurodegenerative activity. TLX activator-1 can be used for the research of neurodegenerative diseases.
For research use only. We do not sell to patients.
- CAS No.: 3108130-51-1
- Formula: C22H18F3N3O2S
- Molecular Weight:445.46
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
TLX activator-1 (Compound 35) (16 h) activates the inhibitory function of TLX in HEK293T cells, with an EC50 of 0.010 μM[1].
At a concentration of 3 μM, TLX activator-1 exhibits a selectivity for TLX that is ≥30-fold higher than that for a panel of nuclear receptors in HEK293T cells, and its IC50 for the inverse agonism of RORα is 8 μM[1].
TLX activator-1 (10 μM; 0-120 min) exhibits high metabolic stability in liver microsomes, with a half-life of 113 min[1].
TLX activator-1 (1 μM; 16 h) exerts anti-neurodegenerative effects by regulating the transcriptome of ARPE-19 cells, which involves upregulating genes related to ATP production, lysosomal function and mitochondrial quality control, while downregulating genes associated with inflammation, apoptosis and amyloidogenic pathways[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3108130-51-1
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Molecular Weight 445.46
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Formula C22H18F3N3O2S
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SMILES
CN(C=C1)C2=C1C=C(C3=CC(C(F)(F)F)=CC(NS(CC4=CC=CC=C4)(=O)=O)=C3)C=N2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
- TLX activator-1
- 3108130-51-1
- TLX activator1
- TLX activator 1
- Orphan Nuclear Receptor
- ATP Synthase
- Apoptosis
- PTEN-induced kinase 1
- ligand-binding domain homodimerization
- RORα
- ARPE-19 cells
- β-secretase
- transcriptional repressor activity
- HEK293T cells
- neurodegenerative diseases
- TLX (NR2E1)
- human liver microsomes
- Inhibitor
- inhibitor
- inhibit