Free shipping on all orders over $ 500

BCTC

Cat. No. M6494
BCTC Structure
Size Price Availability Quantity
5mg USD 80  USD80 In stock
10mg USD 120  USD120 In stock
50mg USD 400  USD400 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
Biological Activity

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.

Protocol
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 372.89
Formula C20H25ClN4O
CAS Number 393514-24-4
Purity 99.96%
Solubility DMSO ≥ 38 mg/mL
Storage at -20°C
References

[1] Tao Liu, et al. Oncol Lett. Anti-tumor activity of the TRPM8 inhibitor BCTC in prostate cancer DU145 cells

[2] Kenneth J Valenzano, et al. J Pharmacol Exp Ther. N-(4-tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a novel, orally effective vanilloid receptor 1 antagonist with analgesic properties: I. in vitro characterization and pharmacokinetic properties

[3] Houlihan, et al. J Neurochem. Activity of cytisine and its brominated isoteres on recombinant human α7, α4β2 and α4β4 nicotinic acetylcholine receptors.

Related TRP Channel Products
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.

  Catalog
Abmole Inhibitor Catalog




Keywords: BCTC supplier, TRP Channel, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.