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480870

Sigma-Aldrich

Neurotrophin Antagonist, Y1036

The Neurotrophin Antagonist, Y1036 controls the biological activity of Neurotrophin. This small molecule/inhibitor is primarily used for Neuroscience applications.

Synonyme(s) :

Neurotrophin Antagonist, Y1036, 3-[4-Oxo-5-[[5-(4-sulfamoylphenyl)-2-furyl]methylene]-2-thioxo-thiazolidin-3-yl]propanoic acid

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About This Item

Formule empirique (notation de Hill):
C17H14N2O6S3
Poids moléculaire :
438.50
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.32

Niveau de qualité

Pureté

≥90% (HPLC)

Forme

solid

Fabricant/nom de marque

Calbiochem®

Conditions de stockage

OK to freeze
protect from light

Couleur

yellow

Solubilité

DMSO: 50 mg/mL

Conditions d'expédition

ambient

Température de stockage

2-8°C

Description générale

A furyl-thioxothiazolidinone compound that binds both BDNF (Cat. No. 203702) and NGF (Cat. No. 480352) (KD = 3.5 and 3.0 µM, respectively) and prevents their interaction with cell surface receptors (IC50 against BDNF/p75NTR, BDNF/trkB, NGF/p75NTR, and NGF/trkA interaction = 6.2, 3.7, 5.7, and 8.8 µM, respectively, in PC12 cultures), while exhibiting no effect against the receptor binding of the non-neurotrophin growth factors EGF and PDGF. Y1036 at 40 µM is shown to inhibit trkA and trkB phosphorylation upon 40 pM BDNF and NGF treatment, respectively, as well as downstream Erk phosphorylation. Y1036 is also demonstrated to block BDNF- and NGF-induced neurite outgrowth in rat embryonic dorsal-root ganglions in a dose-dependent manner.
A furyl-thioxothiazolidinone compound that binds both BDNF (Cat. No. 203702) and NGF (Cat. No. 480352) (KD = 3.5 and 3.0 µM, respectively) and prevents their interaction with cell surface receptors (IC50 against BDNF/p75NTR, BDNF/trkB, NGF/p75NTR, and NGF/trkA interaction = 6.2, 3.7, 5.7, and 8.8 µM, respectively, in PC12 cultures), while exhibiting no effect against the receptor binding of the non-neurotrophin growth factors EGF and PDGF. Y1036 at 40 µM is shown to inhibit trkA and trkB phosphorylation upon 40 pM BDNF and NGF treatment, respectively, as well as downstream Erk phosphorylation. Y1036 is also demonstrated to block BDNF- and NGF-induced neurite outgrowth in rat embryonic dorsal-root ganglions in a dose-dependent manner.

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Autres remarques

Eibl, J.K., et al. 2009. J. Pharmacol. Exp. Ther.332, 446.

Informations légales

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

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 2

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable


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Consulter la Bibliothèque de documents

J K Eibl et al.
The Journal of pharmacology and experimental therapeutics, 332(2), 446-454 (2009-11-20)
Brain-derived neurotrophic factor (BDNF) and nerve growth factor (NGF) are members of the neurotrophin family that normally play a role in the development and maintenance of the nervous system. However, neurotrophin dysregulation has been implicated in several neurodegenerative diseases and

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