ALX 40-4C
| 中文名称 | ALX 40-4C |
|---|---|
| 中文同义词 | AC-D-ARG-D-ARG-D-ARG-D-ARG-D-ARG-D-ARG-D-ARG-D-ARG-D-ARG-NH2;趋化因子受体 (CXCR4) 抑制剂多肽ALX40-4C |
| 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 |
| 结构式 |  |
ALX 40-4C 性质
| 密度 | 1.58±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
|
SDF-1-CXCR4 1 μM (Ki) |
APJ receptor 2.9 μM (IC 50 ) |
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.