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Cyclotraxin B acetate

Cat. No. M14580
Cyclotraxin B acetate Structure
Size Price Availability Quantity
1mg USD 174  USD174 In stock
5mg USD 390  USD390 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 1260.42
Formula C50H77N13O19S3
CAS Number 1203586-72-4(free base)
Solubility (25°C) Water 90 mg/mL
Storage -20°C, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] P Totoson, et al. Endothelial TrkB receptor activation controls vascular tone of rat middle cerebral artery

[2] Jeffri Retamal, et al. Burst-Like Subcutaneous Electrical Stimulation Induces BDNF-Mediated, Cyclotraxin B-Sensitive Central Sensitization in Rat Spinal Cord

[3] Calais S Prince, et al. Tropomyosin Receptor Kinase B Agonist, 7,8-Dihydroxyflavone, Improves Mitochondrial Respiration in Placentas From Obese Women

[4] 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

[5] Maxime Cazorla, et al. Cyclotraxin-B, the first highly potent and selective TrkB inhibitor, has anxiolytic properties in mice

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Keywords: Cyclotraxin B acetate supplier, Trk, inhibitors, activators

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