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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 |
|---|
| 4-(Phenylazo)benzoic acid
4-(Phenyldiazenyl)benzoic acid is a photosensitive and photoswitchable TRPA1 agonist that can be used for the research of pain signaling. |
| Podocarpic acid
Podocarpic acid is a natural product, which acts as a novel TRPA1 activator. |
| Vocacapsaicin hydrochloride
Vocacapsaicin (CA-008) hydrochloride, as a prodrug of capsaicin, is the first non-opioid TRPV1 agonist. Vocacapsaicin hydrochloride provides lasting pain relief. |
| Vocacapsaicin
Vocacapsaicin (CA-008), a prodrug of capsaicin, is the first (first-in-class) non-opioid TRPV1 agonist. Vocacapsaicin can provide lasting pain relief. |
| GDC-0334
GDC-0334 is a TRPA1 antagonist for the treatment of TRPA1-mediated disease and is an oral candidate compound for the study of asthma. |
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