1. GPCR/G Protein Immunology/Inflammation
  2. CXCR Apelin Receptor (APJ)
  3. ALX 40-4C Trifluoroacetate

ALX 40-4C Trifluoroacetate is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.

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ALX 40-4C Trifluoroacetate

ALX 40-4C Trifluoroacetate Estructura química

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Based on 1 publication(s) in Google Scholar

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Descripciòn

ALX 40-4C Trifluoroacetate is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM.

IC50 & Target[1][3]

SDF-1-CXCR4

1 μM (Ki)

APJ receptor

2.9 μM (IC50)

In Vitro

ALX 40-4C Trifluoroacetate is a small peptide inhibitor of the chemokine receptor CXCR4, interacts with the second extracellular loop of CXCR4 and inhibits infection exclusively by blocking direct virus-CXCR4 interactions[1]. ALX 40-4C shows potent anti HIV-1 effect, with EC50s of 0.34 ± 0.04 μg/mL, 0.37 ± 0.01 μg/mL for HIV-1 NL4-3, NC10, and 0.18 ± 0.11 μg/mL, 0.06 ± 0.02 μg/mL for HIV-1 HXB2, HC43, respectively, and with a CC50 (50% cytotoxic concentration) of 21 μg/mL. ALX 40-4C also exhibits potent activity against env-recombinant HIV, with EC50s of 0.38 ± 0.01 μg/mL, 0.40 ± 0.0 μg/mL for HIV-1 NL4-3 env, NC10, and 1.34 ± 0.06 μg/mL, 1.02 ± 0.29 μg/mL for HIV-1 HXB2 env, HC43, and a CC50 of 21 μg/mL[2]. ALX 40-4C binds to APJ with an IC50 of 2.9 μM. ALX 40-4C inhibits HIV-1 gp120/APJ-mediated cell membrane fusion, with an IC50s of 3.41 μM and 3.1 μM for IIIB isolate and 89.6 isolate, respectively[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Peso molecular

1464.74 (free base)

Fòrmula

C56H113N37O10.xC2HF3O2

Appearance

Solid

Color

White to off-white

Sequence

Ac-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-NH2

Sequence Shortening

Ac-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-{d-Arg}-NH2

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvente y solubilidad
In Vitro: 

H2O : 50 mg/mL (Need ultrasonic)

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Pureza y Documentación
Referencias
Ensayo de quinasas
[3]

The stably transfected cells are harvested in PBS (Ca2+ and Mg2+ free) plus 0.5 nM EDTA and washed twice with PBS. Ligand binding experiments are performed using a single concentration (0.2 nM) of 125I-Apelin-13 in the absence or presence of increasing concentrations of unlabeled Apelin-13 or ALX 40-4C in a final volume of 100 μL of binding buffer (50 nM Hepes, pH 7.4, 1 nM CaCl2, 5 nM MgCl2, 0.1% bovine serum albumin) containing 5 × 105 cells. Nonspecific binding is determined by the addition of 1 μM unlabeled Apelin-13. Samples are incubated for 90 min at room temperature. The incubation is terminated by separating the cells from the binding buffer by centrifugation and washing once with 500 μL of cold binding buffer. Bound ligands are determined by counting gamma emissions. At least three independent experiments are performed[3].

MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

Nombre del producto:
ALX 40-4C Trifluoroacetate
Cat. No.:
HY-P7061A
Cantidad:
MCE Japan Authorized Agent: