ALX 40-4C | Cytiva思拓凡-Whatman滤纸滤膜滤器

ALX 40-4C;

ALX 40-4C 是一种趋化因子受体 (CXCR4) 抑制剂，能够抑制 SDF-1 与 CXCR4 结合，K_i 值为 1 μM，具有抗 HIV-1 作用；ALX 40-4C Trifluoroacetate 同时为 APJ 受体拮抗剂，IC₅₀ 值为 2.9 μM。

ALX 40-4C Chemical Structure

CAS No. : 143413-49-4

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ALX 40-4C 的其他形式现货产品:

ALX 40-4C Trifluoroacetate

生物活性

ALX 40-4C is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a K_i 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

SDF-1-CXCR4

1 mu;M (Ki)

APJ receptor

2.9 mu;M (IC₅₀)

体外研究
(In Vitro)

ALX 40-4C 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].

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

分子量

1464.74

Formula

C₅₆H₁₁₃N₃₇O₁₀

CAS 号

143413-49-4

Sequence Shortening

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

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Doranz BJ, et al. Safe use of the CXCR4 inhibitor ALX40-4C in humans. AIDS Res Hum Retroviruses. 2001 Apr 10;17(6):475-86.

[2]. Armand-Ugón M, et al. HIV-1 resistance to the gp41-dependent fusion inhibitor C-34. Antiviral Res. 2003 Jul;59(2):137-42.

[3]. Zhou N, et al. Binding of ALX40-4C to APJ, a CNS-based receptor, inhibits its utilization as a co-receptor by HIV-1. Virology. 2003 Jul 20;312(1):196-203.

Kinase Assay ^[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 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Doranz BJ, et al. Safe use of the CXCR4 inhibitor ALX40-4C in humans. AIDS Res Hum Retroviruses. 2001 Apr 10;17(6):475-86. [2]. Armand-Ugón M, et al. HIV-1 resistance to the gp41-dependent fusion inhibitor C-34. Antiviral Res. 2003 Jul;59(2):137-42. [3]. Zhou N, et al. Binding of ALX40-4C to APJ, a CNS-based receptor, inhibits its utilization as a co-receptor by HIV-1. Virology. 2003 Jul 20;312(1):196-203.

Kinase Assay
^[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 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

[1]. Doranz BJ, et al. Safe use of the CXCR4 inhibitor ALX40-4C in humans. AIDS Res Hum Retroviruses. 2001 Apr 10;17(6):475-86.

[2]. Armand-Ugón M, et al. HIV-1 resistance to the gp41-dependent fusion inhibitor C-34. Antiviral Res. 2003 Jul;59(2):137-42.

[3]. Zhou N, et al. Binding of ALX40-4C to APJ, a CNS-based receptor, inhibits its utilization as a co-receptor by HIV-1. Virology. 2003 Jul 20;312(1):196-203.