ALX 40-4C

中文名称:

ALX 40-4C

中文同义词:

英文名称:

ALX 40-4C

英文同义词:

ALX 40-4C;D-Argininamide, N2-acetyl-D-arginyl-D-arginyl-D-arginyl-D-arginyl-D-arginyl-D-arginyl-D-arginyl-D-arginyl- (9CI)

CAS号:

143413-49-4

分子式:

C56H113N37O10

分子量:

1464.74

EINECS号:

相关类别:

多肽合成定制;多肽

Mol文件:

143413-49-4.mol

密度 

1.58±0.1 g/cm3(Predicted)

生物活性

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，Ki 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。

靶点

SDF-1-CXCR4 1 μM (Ki) APJ receptor 2.9 μM (IC 50 )

SDF-1-CXCR4 1 μM (Ki)

APJ receptor 2.9 μM (IC 50 )

体外研究

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. ALX 40-4C shows potent anti HIV-1 effect, with EC 50 s 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 CC 50 (50% cytotoxic concentration) of 21 μg/mL. ALX 40-4C also exhibits potent activity against env-recombinant HIV, with EC 50 s 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 CC 50 of 21 μg/mL. ALX 40-4C binds to APJ with an IC 50 of 2.9 μM. ALX 40-4C inhibits HIV-1 gp120/APJ-mediated cell membrane fusion, with an IC 50 s of 3.41 μM and 3.1 μM for IIIB isolate and 89.6 isolate, respectively.