In vitro: 7,8-DHF is one of the positive compounds that specifically activate TrkB, but not TrkA or TrkC, at a concentration of 250 nM. In addition to cortical and hippocampal neurons, 7,8-DHF also protects other cell types including the RGC (retinal ganglion cells) and PC12 cells from excitotoxic and oxidative stress-induced apoptosis and cell death. Thus, it has neuroprotective properties. In vivo: 7,8-Dihydroxyflavone is a bioavailable chemical that can pass through the BBB to provoke TrkB and its downstream PI3K/Akt and MAPK activation in mouse brain upon intraperitoneal or oral administration. 7,8-DHF promotes the survival and reduces apoptosis in cortical neurons of traumatic brain injury as administration of 7,8-DHF at 3 h post-injury reduces brain tissue damage via the PI3K/Akt pathway. Its treatment does not induce any apparent toxicity in mice and is not toxic to the mice during the chronic treatment. 7,8-DHF displays robust therapeutic efficacy toward Alzheimer's disease and inhibits obesity through activating muscular TrkB.
| Molecular Weight | 254.24 |
| Formula | C15H10O4 |
| CAS Number | 38183-03-8 |
| Form | Solid |
| Solubility (25°C) | 50 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Trk Products |
|---|
| Cyclotraxin B
Cyclotraxin B, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. |
| Gambogic amide
Gambogic amide is a potent and selective agonist of TrkA and also induces its tyrosine phosphorylation and activation of downstream signaling, including Akt and MAPK. |
| Protein kinase inhibitor 4
Protein kinase inhibitor 4 is a protein kinase inhibitor that inhibits TRK-A and ROS1 (IC50=3.0 nM and 104 nM respectively). |
| TRK-IN-22
TRK-IN-22 is a TRK inhibitor. |
| TrkB-IN-1
TrkB-IN-1 is a potent and orally active TrkB agonist and has favorable PK properties. |
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