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.
| Related Trk Products |
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| Anizatrectinib
Anizatrectinib (hTrkA-IN-1) is a potent and orally active inhibitor of TrkA kinase with an IC50 of 1.3 nM. Anizatrectinib can be used for the study of inflammatory disease, such as prostatitis, pelvic, et al. |
| Bedinvetmab
Bedinvetmab (ZTS-00508841) is a canine monoclonal antibody (mAb) targeting nerve growth factor (NGF). Bedinvetmab inhibits NGF interaction with tropomyosin receptor kinase A (trkA) and p75 neurotrophin receptor (p75NTR) receptors. Bedinvetmab can be used for the research of osteoarthritis pain in dogs. |
| CG428
CG428 is a TRK kinase fusion protein degrader. |
| Tavilermide
Tavilermide is a selective, partial agonist of TrkA, or a nerve growth factor (NGF) mimetic. |
| AZ-23
AZ-23 is an ATP-competitive and orally bioavailable Trk kinase A/B/C inhibitor with IC50s of 2 nM (TrkA), 8 nM (TrkB), 24 nM (FGFR1), 52 nM (Flt3), 55 nM (Ret), 84 nM (MuSk), 99 nM (Lck), respectively. |
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