5.30615

GFRα/RET Signaling Activator, XIB-4035

• Synonyme(s) : GFRα/RET Signaling Activator, XIB-4035, ( E)-N⁴-(7-Chloro-2-(2-chlorostyryl)quinolin-4-yl)-N¹,N¹-diethylpentane-1,4-diamine, N-(7-Chloro-2-(2-(2-chlorophenyl)vinyl)-4-quinolinyl)-N-(4-(diethylamino)-1-methylbutyl)amine, XIB 4035
• Formule empirique (notation de Hill): C₂₆H₃₁Cl₂N₃
• Numéro CAS: 10023-54-8
• Poids moléculaire : 456.45
• Code UNSPSC : 12352200

Propriétés

• Pureté: ≥97% (HPLC)
• Niveau de qualité: 100
• Forme: powder
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: yellow
• Solubilité: DMSO: 100 mg/mL
• Température de stockage: −20°C
• InChI: 1S/C26H31Cl2N3/c1-4-31(5-2)16-8-9-19(3)29-26-18-22(14-12-20-10-6-7-11-24(20)28)30-25-17-21(27)13-15-23(25)26/h6-7,10-15,17-19H,4-5,8-9,16H2,1-3H3,(H,29,30)/b14-12+
• Clé InChI: CMLVHSVFSYNMGM-WYMLVPIESA-N

Description

Description générale

A cell-permeable chlorostyrylquinolinylbutylamino compound that was shown to competitively bind to glial cell line-derived neurotrophic factor (GDNF) family receptor-α1 (GFRα1) and act as an agonist (IC₅₀ = 10.4 µM for ¹²⁵I-GDNF binding in Neuro-2A cells) and induce autophosphorylation of RET protein. Elicits neurite outgrowth of Neuro-2A cells in a dose-dependent manner. However, some of the recent studies have questioned its agonist nature and have suggested that it acts as a positive modulator of ligand-Induced GFRα/RET signaling and prolongs the GDNF-induced RET phosphorylation. Shown to be effective in treating small fiber neuropathy caused by non-myelinating Schwann cell dysfunction in diabetic murine models leading to improved thermononiception. Does not appear to be toxic up to ~100 µM.

A cell-permeable chlorostyrylquinolinylbutylamino compound that was shown to competitively bind to glial cell line-derived neurotrophic factor (GDNF) family receptor-α1 (GFRα1) and act as an agonist (IC₅₀ = 10.4 µM for ¹²⁵I-GDNF binding in Neuro-2A cells) and induce autophosphorylation of RET protein. Elicits neurite outgrowth of Neuro-2A cells in a dose-dependent manner. However, some of the recent studies have questioned its agonist nature and have suggested that it acts as a positive modulator of ligand-Induced GFRα/RET signaling and prolongs the GDNF-induced RET phosphorylation. Shown to be effective in treating small fiber neuropathy caused by non-myelinating Schwann cell dysfunction in diabetic murine models leading to improved thermononiception. Does not appear to be toxic up to ~100 µM.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
GFRα1

Reversible: yes

Target IC₅₀: 10.4 µM for ¹²⁵I-GDNF binding in Neuro-2A cells

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 3 months at -20°C.

Use only fresh DMSO for reconstitution.

Autres remarques

Hedstrom, K.L., et al. 2014. Proc. Natl. Acad. Sci. USA111, 2325.
Tokugawa, K., et al. 2003. Neurochem. Int.42, 81.

Informations légales

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

Informations sur la sécurité

• Pictogrammes: GHS06
• Mention d'avertissement: Danger
• Mentions de danger: H301 - H413
• Conseils de prudence: P264 - P270 - P273 - P301 + P310 - P405 - P501
• Classification des risques: Acute Tox. 3 Oral - Aquatic Chronic 4
• Code de la classe de stockage: 6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable