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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.
| 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 |
| Related TRP Channel Products |
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| TRPM4-IN-1
Trpm4-in-1 (CBA) is an effective and selective cationic channel TRPM4 inhibitor with an IC50 of 1.5 μM. |
| GFB-8438
GFB-8438 is a potent subtype selective TRPC5 inhibitor against hTRPC5 and hTRPC4 IC50 0.18 and 0.29 μM, respectively. GFB-8438 has good selectivity for TRPC6, other members of the TRP family, NaV1.5, and limited activity against hERG channels. Protective effect of GFB-8438 on mouse podocytes. |
| Mavatrep
Mavatrep is an orally active TRPV1 antagonist with high affinity for the hTRPV1 channel, inhibits the binding of the TRPV1 agonist to [3H]-Resiniferatoxin (Ki=6.5 nM), and has a low effect on the enzymatic activity of CYP subtypes 3A4, 1A2, and 2D6. |
| JNJ-17203212
JNJ-17203212 is a selective, highly effective, competitive TRPV1 antagonist. JNJ-17203212 was developed for research on pain management, such as migraines. |
| Asivatrep
Asivatrep (PAC-14028) is a highly selective transient receptor potential vanilla acid subtype 1 (TRPV1) antagonist. |
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