5.30615

GFRα/RET Signaling Activator, XIB-4035

• 別名: 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
• 実験式（ヒル表記法）: C₂₆H₃₁Cl₂N₃
• CAS番号: 10023-54-8
• 分子量: 456.45
• UNSPSCコード: 12352200

特性

• アッセイ: ≥97% (HPLC)
• 品質水準: 100
• フォーム: powder
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: yellow
• 溶解性: DMSO: 100 mg/mL
• 保管温度: −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+
• InChI Key: CMLVHSVFSYNMGM-WYMLVPIESA-N

詳細

詳細

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.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
GFRα1

Reversible: yes

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

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

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.

その他情報

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

法的情報

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

安全性情報

• ピクトグラム: GHS06
• シグナルワード: Danger
• 危険有害性情報: H301 - H413
• 注意書き: P264 - P270 - P273 - P301 + P310 - P405 - P501
• 危険有害性の分類: Acute Tox. 3 Oral - Aquatic Chronic 4
• 保管分類コード: 6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable