5.06304

ANA-12

≥98% (HPLC), TrkB antagonist, solid

• Synonyma: TrkB Antagonist, ANA-12, N-(2-((2-oxoazepan-3-yl)carbamoyl)phenyl)benzo[b]thiophene-2-carboxamide
• Empirický vzorec (Hillův zápis): C₂₂H₂₁N₃O₃S
• Číslo CAS: 219766-25-3
• Molekulová hmotnost: 407.49
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD00117444
• Assay: ≥98% (HPLC)
• Form: solid
• Quality level: 100
• Storage condition: OK to freeze, protect from light

Vlastnosti

• Název produktu: 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
• SMILES string: [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)
• InChI key: TUSCYCAIGRVBMD-UHFFFAOYSA-N

Popis

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

Preparation Note

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.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Bezpečnostní informace

• pictograms: GHS07
• signalword: Warning
• hcodes: H302
• pcodes: P264 - P270 - P301 + P312 - P501
• Hazard Classifications: Acute Tox. 4 Oral
• Skladovací třída: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable