5.06304

TrkB Antagonist, ANA-12

• Sinônimo(s): TrkB Antagonist, ANA-12, N-(2-((2-oxoazepan-3-yl)carbamoyl)phenyl)benzo[b]thiophene-2-carboxamide
• Fórmula empírica (Notação de Hill): C₂₂H₂₁N₃O₃S
• Número CAS: 219766-25-3
• Peso molecular: 407.49
• Número MDL: MFCD00117444
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Ensaio: ≥98% (HPLC)
• Nível de qualidade: 100
• Formulário: solid
• potência: 10 nM K_i
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: white
• solubilidade: DMSO: 25 mg/mL
• temperatura de armazenamento: 2-8°C
• cadeia de caracteres SMILES: [s]1c2c(cc1C(=O)Nc3c(cccc3)C(=O)NC4CCCCNC4=O)cccc2
• 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)
• chave InChI: TUSCYCAIGRVBMD-UHFFFAOYSA-N

Descrição

Descrição geral

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.

Ações bioquímicas/fisiológicas

Primary Target
TrkB

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Reconstituição

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

Outras notas

Cazorla, M., et al. 2011. J. Clin. Invest.121,1846.

Informações legais

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informações de segurança

• Pictogramas: GHS07
• Palavra indicadora: Warning
• Frases de perigo: H302
• Declarações de precaução: P264 - P270 - P301 + P312 - P501
• Classificações de perigo: Acute Tox. 4 Oral
• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable