T-448 free base
T-448 free base is a specific, orally active, CNS-penetrant and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 free base enhances H3K4 methylation in primary cultured rat neurons.
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- CAS. Nr.: 1597426-52-2
- Formel: C17H20N4OS
- Molecular Weight:328.43
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
IC50 & Target
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KDM1/LSD1 |
In Vitro
T-448 enhances the levels of H3K4 methylation, increased mRNA expression of neural plasticity-related genes including brain derived neurotrophic factor (Bdnf), and ameliorated learning dysfunction[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Primary cultured rat neurons.
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Concentration:0-10 μM.
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Incubation Time:1 day treatment.
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Result:Increased Ucp2 H3K4me2 and Ucp2 mRNA significantly.
In Vivo
T-448 increases H3K4 methylation in the brain without causing hematological side effects even at 100 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NR1-hypo mice[1].
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Dosage:1, 10 mg/kg.
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Administration:Orally, 3 weeks.
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Result:Dose-dependently increased the H3K4me2 levels around Bdnf, Arc, and Fos genes in the mouse hippocampus.
Resulted in partial but statistically significant and dosedependent rescue effects on the rate of correct choices in NR1-hypo mice.
Chemical Information
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CAS. Nr. 1597426-52-2
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Molecular Weight 328.43
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Formel C17H20N4OS
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SMILES
O=C(NC1=NN=C(C)S1)C2=CC=CC([C@H]3[C@H](NC4CCC4)C3)=C2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)