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.
|CAS Number||1203586-72-4(free base)|
|Solubility (25°C)||Water 90 mg/mL|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
 Luis Constandil, et al. Cyclotraxin-B, a new TrkB antagonist, and glial blockade by propentofylline, equally prevent and reverse cold allodynia induced by BDNF or partial infraorbital nerve constriction in mice
|Related Trk Products|
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 (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 is a TRK kinase fusion protein degrader.
Tavilermide is a selective, partial agonist of TrkA, or a nerve growth factor (NGF) mimetic.
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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