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.
Evid Based Complement Alternat Med. 2022 Apr 13;2022:5731372.
Gallic Acid Inhibits Mesaconitine-Activated TRPV1-Channel-Induced Cardiotoxicity
BCTC purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| 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. |
| Molecular Weight | 372.89 |
| Formula | C20H25ClN4O |
| CAS Number | 393514-24-4 |
| Solubility (25°C) | DMSO ≥ 38 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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 TRP Channel Products |
|---|
| beta-Eudesmol
Beta-Eudesmol is a natural oxygenated sesquiterpene, activates hTRPA1, with an EC50 of 32.5 μM. Beta-Eudesmol increases appetite through TRPA1. |
| GFB-887
GFB-887 is an inhibitor of transient receptor potential channels 4 and 5 (TRPC4/5) and can be used in studies related to anxiety disorders. |
| Tivanisiran
Tivanisiran is an siRNA that silences TRPV1 mRNA and can be used in studies related to dry eye. |
| MK-2295
MK-2295 (NGD-8243) is a TRPV1 antagonist. |
| KM-001
KM-001 is a potent and selective TRPV3 antagonist. |
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