ALX 40-4C acetate 是趋化因子受体 (Ki = 1 μM) 的 CXCR4 抑制剂,可抑制 HIV-1 X4 株的复制。 ALX 40-4C acetate 是 APJ 受体的拮抗剂 (IC50 = 2.9 μM)。
产品描述
ALX 40-4C acetate is a CXCR4 inhibitor of the chemokine receptor (Ki = 1 μM) and suppresses the replication of X4 strains of HIV-1. ALX 40-4C acetate is an antagonist of the APJ receptor (IC50 = 2.9 μM).
体外活性
ALX 40-4C acetate 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 acetate 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[1]. ALX 40-4C acetate binds to APJ with an IC50 of 2.9 μM. ALX 40-4C acetate 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[2].
Cas No.
TP1364L
分子式
C58H117N37O12
分子量
1524.79
别名
ALX 40-4C acetate(143413-49-4 free base)
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years