| Identification | Back Directory | [Name]
4H-1-Benzopyran-4-one, 7,8-bis[[(methylamino)carbonyl]oxy]-2-phenyl- | [CAS]
1609067-49-3 | [Synonyms]
TrkB-IN-1
TrkB agonist prodrug R13
4H-1-Benzopyran-4-one, 7,8-bis[[(methylamino)carbonyl]oxy]-2-phenyl- | [Molecular Formula]
C19H16N2O6 | [MOL File]
1609067-49-3.mol | [Molecular Weight]
368.34 |
| Chemical Properties | Back Directory | [Boiling point ]
545.7±50.0 °C(Predicted) | [density ]
1.353±0.06 g/cm3(Predicted) | [solubility ]
Acetonitrile: Slightly soluble: 0.1-1 mg/ml
DMSO: Slightly soluble: 0.1-1 mg/ml
Water: Slightly soluble: 0.1-1 mg/ml | [pka]
11.22±0.46(Predicted) |
| Hazard Information | Back Directory | [Uses]
TrkB-IN-1 is a potent and orally active TrkB agonist and has favorable PK properties. TrkB-IN-1 reverses the cognitive defects in an AD mouse model and can be used for alzheimer’s disease research[1]. | [in vivo]
TrkB-IN-1 (oral gavage; 7.25 mg/kg, 21.8 mg/kg, 43.6 mg/kg; 3 month) activates TrkB signaling cascade in the hippocampus of 5XFAD mice in a dose-dependent manner in 5XFAD mice, the ratio of p-TrkB/TrkB, p-Akt/Akt and p-ERK/ERK is also increased[1].
TrkB-IN-1 (oral gavage; 7.25 mg/kg, 21.8 mg/kg, 43.6 mg/kg; 5 days) alleviates Aβ deposition and rescues memory deficits in 5XFAD mice[1].
TrkB-IN-1 (oral gavage; 36 mg/kg) exhibits ～10.5% oral bioavailability with a Cmax?of 129 ng/mL, Tmax?of 0.5 h, and T1/2?for oral administration of 3.66 h[1]. | [IC 50]
TrkB | [References]
[1] Chun Chen, et al. The prodrug of 7,8-dihydroxyflavone development and therapeutic efficacy for treating Alzheimer's disease. Proc Natl Acad Sci U S A. 2018 Jan 16;115(3):578-583. DOI:10.1073/pnas.1718683115 |
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Biorbyt Ltd.
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+44 (0)1223 859 353 |
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http://www.biorbyt.com |
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