Cyclotraxin B acetate, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B non-competitively inhibits BDNF-induced TrkB activity with an IC50 of 0.30 nM. Cyclotraxin B acetate can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects.
Molecular Weight | 1260.42 |
Formula | C50H77N13O19S3 |
CAS Number | 1203586-72-4(free base) |
Solubility (25°C) | Water 90 mg/mL |
Storage | -20°C, sealed |
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.
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Cyclotraxin B
Cyclotraxin B, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. |
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