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Key Documents

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.

Sinónimos:

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

Fórmula empírica (notación de Hill):
C17H14N2O6S3
Peso molecular:
438.50
UNSPSC Code:
12352200
NACRES:
NA.32

Quality Level

assay

≥90% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

yellow

solubility

DMSO: 50 mg/mL

shipped in

ambient

storage temp.

2-8°C

General description

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.

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 6 months at -20°C.

Other Notes

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

Legal Information

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable


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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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