BCTC is a orally effective vanilloid receptor 1 (TRPV1 receptor) antagonist. BCTC is also a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells. BCTC inhibits acid- and capsaicin-induced activation of rat TRPV1 receptors (IC50 values are 6.0 and 35 nM respectively). BCTC displays analgesic properties in rat models of inflammatory and neuropathic pain.
Cell Experiment | |
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Cell lines | |
Preparation method | |
Concentrations | |
Incubation time |
Animal Experiment | |
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Animal models | Jugular-cannulated male Sprague-Dawley rats (200-300 g) |
Formulation | using 25% hydroxypropyl-β-cyclodextrin as vehicle |
Dosages | 3, 10, and 40 mg/kg p.o. or 3 mg/kg i.v. |
Administration | p.o. or i.v. |
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.
Molecular Weight | 372.89 |
Formula | C20H25ClN4O |
CAS Number | 393514-24-4 |
Purity | 99.96% |
Solubility | DMSO ≥ 38 mg/mL |
Storage | at -20°C |
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