239825

AMD3100

InSolution, ≥98%, 50 mM aqueous solution, CXCR4 antagonist I

• Sinónimos: InSolution CXCR4 Antagonist I, AMD3100, 1,1ʹ(1,4-Phenylenebis(methylene))-bis-1,4,8,11-tetraazacyclotetradecane, 8HCl, 4H₂O, 1,4-bis((1,4,8,11-Tetraazacyclotetradecan-1-yl)methyl)benzene, 8HCl, 4H₂O
• Fórmula empírica (notación de Hill): C₂₈H₅₄N₈ · 8HCl · 4H₂O
• Número de CAS: 155148-31-5
• Peso molecular: 866.53
• Código UNSPSC: 51111800
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Análisis: ≥98% (HPLC)
• formulario: liquid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; avoid repeated freeze/thaw cycles; protect from light
• Condiciones de envío: dry ice
• temp. de almacenamiento: −70°C
• InChI: 1S/C28H54N8.8ClH/c1-9-29-15-17-31-13-3-21-35(23-19-33-11-1)25-27-5-7-28(8-6-27)26-36-22-4-14-32-18-16-30-10-2-12-34-20-24-36;;;;;;;;/h5-8,29-34H,1-4,9-26H2;8*1H
• Clave InChI: UEUPDYPUTTUXLJ-UHFFFAOYSA-N

Descripción

Descripción general

A symmetrical bicyclam compound that antagonizes CXCL12 (SDF1) binding to CXCR4 (IC₅₀ = 108 and 245 nM using rat and human CXCR4, respectively) and inhibits SDF1-induced Ca²⁺ flux (by 100% at 100 ng/ml in SUP-T1 and THP-1 cultures) as well as CXCR4-, but not CCR5-, mediated HIV infection (IC₅₀ = 200 nM), while enhancing the binding of SDF1 to CXCR7 (by ~60% at 1 mM with CXCR7-expressing HEK293T cells) and SDF1-induced β-arrestin recruitment to CXCR7 (EC₅₀ = 6.48 and 11.8 nM, in the presence and absence of 10 µM AMD3100, respectively). Administration AMD3100 via intravenous infusion is also reported to result in hematopoietic stem cell mobilization in humans, dogs, and mice in vivo. Exhibits no inhibitory effects against chemokine-induced signaling via CXCR1/2/3 or CCR1/2/3/4/5/6/7/8/9.

Acciones bioquímicas o fisiológicas

Cell permeable: yes

Primary Target
CXCR4

Reversible: yes

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Forma física

A 50 mM (15 mg/308 µL) solution of CXCR4 Antagonist I, AMD3100 (Cat. No. 239820) in H₂O.

Reconstitución

Following initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 1 year at -70°C.

Otras notas

Kalatskaya, I., et al. 2009. Mol. Pharmacol.77, 1240.
Pitchford, S.C., et al. 2009. Cell Stem Cell4, 62.
De Clercq, E. 2009. Biochem. Pharmacol.77, 1655.
Thoma, G., et al. 2008. J. Med. Chem.51, 7915.
De Clercq, E. 2000. Mol. Pharmacol.57, 833.

Información legal

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

Información de seguridad

• Código de clase de almacenamiento: 10 - Combustible liquids
• Clase de riesgo para el agua (WGK): WGK 3