Sigma-Aldrich Trkb Antagonist Ana-12

Assay

≥98% (HPLC)

Quality Level

100

Form

solid

Potency

10 nM K_i

Manufacturer/Tradename

Calbiochem^®

Storage Condition

OK to freeze
protect from light

Color

white

Solubility

DMSO: 25 mg/mL

Storage Temp.

2-8°C

Inchi

1S/C22H21N3O3S/c26-20(25-17-10-5-6-12-23-21(17)27)15-8-2-3-9-16(15)24-22(28)19-13-14-7-1-4-11-18(14)29-19/h1-4,7-9,11,13,17H,5-6,10,12H2,(H,23,27)(H,24,28)(H,25,26)

General Description

A cell-permeable thiophene carboxymide derived compound that acts as a direct and selective antagonist of TrkB receptor. Binds to the high affinity site on the extracellular domain of TrkB in a dose-dependent manner (K_d= 10 nM) exhibiting much reduced binding to the low affinity site (K_d=12 µM) indicating that it does not compete with BDNF for the same binding site. Does not affect TrkA or TrkC receptors. Shown to permeate the blood-brain barrier, however, its antagonistic effects are not uniform throughout the brain. Does not affect the survivability of neurons. Reduces anxiety and depression related behavior in mice.

Biochem/Physiol Actions

Primary Target
TrkB

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Cazorla, M., et Al. 2011.J. Clin. Invest. 121,1846.CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, GermanyGHS07H302P264 - P270 - P301 + P312 - P501