5.30615

GFRα/RET Signaling Activator, XIB-4035

• Sinonimo/i: 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
• Formula empirica (notazione di Hill): C₂₆H₃₁Cl₂N₃
• Numero CAS: 10023-54-8
• Peso molecolare: 456.45
• Codice UNSPSC: 12352200

Proprietà

• Saggio: ≥97% (HPLC)
• Livello qualitativo: 100
• Forma fisica: powder
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: yellow
• Solubilità: DMSO: 100 mg/mL
• Temperatura di conservazione: −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+; CMLVHSVFSYNMGM-WYMLVPIESA-N

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
GFRα1

Reversible: yes

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

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

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.

Altre note

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

Note legali

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

Informazioni sulla sicurezza

• Pittogrammi: GHS06
• Avvertenze: Danger
• Indicazioni di pericolo: H301 - H413
• Consigli di prudenza: P264 - P270 - P273 - P301 + P310 - P405 - P501
• Classi di pericolo: Acute Tox. 3 Oral - Aquatic Chronic 4
• Codice della classe di stoccaggio: 6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable