5.00507

CXCR4 Antagonist IV, TF14016

• Sinónimos: CXCR4 Antagonist IV, TF14016, Fusin Antagonist IV
• Fórmula empírica (notación de Hill): C₁₀₁H₁₄₅FN₃₄O₁₈S₂ · xH₂O
• Peso molecular: 2206.58 (anhydrous basis)
• Código UNSPSC: 51111800
• NACRES: NA.77

Propiedades

• Ensayo: ≥95% (HPLC)
• Nivel de calidad: 100
• Formulario: solid
• potencia: 0.9 nM IC₅₀
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: white
• solubilidad: H₂O: 100 mg/mL
• temp. de almacenamiento: −20°C

Descripción

Descripción general

A 14-aa internally disulfide-bonded peptide that potently competes against SDF-1α/CXCL12 for CXCR4 binding (IC₅₀ = 0.91 nM; [SDF-1] = 100 nM) and protects MT-4 cells against X4-HIV strain HIV-1_IIIB infection (EC₅₀ = 4 nM in 5 d; MOI = 0.01) with no significant cytotoxicity (CC₅₀ = 56 µM; 5 d). Inhibits SDF-1-induced Ca²⁺ mobilization (IC₅₀ = 4.5 nM; [SDF-1] = 30 nM; CXCR4-expressing CHO cells) in vitro and effectively prevents CXCR4-dependent 5BC-5 metastasis in NK-depleted SCID mice in vivo (10 mg/kg i.p.) in vivo.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Acciones bioquímicas o fisiológicas

Cell permeable: yes

Primary Target
CXCR4

Advertencia

Toxicity: Standard Handling (A)

Secuencia

N^α-4-fluorobenzoyl-Arg-Arg-Nal-Cys⁴-Tyr-Cit-Lys-D-Lys-Pro-Tyr-Arg-Cit-Cys¹³-Arg-NH₂ (Disulfide bond: 4 → 13; Nal = L-3-(2-naphthyl)alanine; Cit = L-citrulline)

Forma física

Supplied as a trifluoroacetate salt.

Reconstitución

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Otras notas

Otani, Y., et al. 2012. FEBS Lett.586, 3639.
Oishi, S., and Fujii, N. 2012. Org. Biomol. Chem.10, 5720.
Tamamura, H., et al. 2003. Org. Biomol. Chem.1 3663.
Tamamura, H., et al. 2003. Org. Biomol. Chem.1, 3656.

Información legal

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

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 1
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable