5.30615

GFRα/RET Signaling Activator, XIB-4035

• 동의어(들): 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
• 실험식(Hill 표기법): C₂₆H₃₁Cl₂N₃
• CAS Number: 10023-54-8
• Molecular Weight: 456.45
• UNSPSC 코드: 12352200

속성

• 분석: ≥97% (HPLC)
• Quality Level: 100
• 양식: powder
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: yellow
• solubility: DMSO: 100 mg/mL
• 저장 온도: −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

설명

일반 설명

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.

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
GFRα1

Reversible: yes

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

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

재구성

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.

기타 정보

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

법적 정보

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

안전성 정보

• 픽토그램: GHS06
• 신호어: Danger
• 유해 및 위험 성명서: H301 - H413
• 예방조치 성명서: P264 - P270 - P273 - P301 + P310 - P405 - P501
• Hazard Classifications: Acute Tox. 3 Oral - Aquatic Chronic 4
• Storage Class Code: 6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable