ZLM-66 是一种有效的non-nucleoside Reverse Transcriptase抑制剂 (NNRTIs)，对野生型HIV-1逆转录酶的IC50值为 41 nM，对野生型 HIV-1 的EC50值为 13 nM。ZLM-66 是一种多拉维林 (Doravirine) 类似物。ZLM-66 可用于艾滋病 (AIDS) 的研究。
产品描述
ZLM-66 is a potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) with an IC 50 of 41 nM for wild-type (WT) HIV-1 reverse transcriptase and an EC 50 value of 13 nM for wild-type HIV-1. ZLM-66 is a Doravirine analogs. ZLM-66 can be used for the research of AIDS [1].
体外活性
ZLM-66 (0.0016-125 μg/ml, 5 d) inhibits HIV-1 and HIV-1 mutant strains in MT-4 cells [1]. Cell Viability Assay [1] Cell Line: MT-4 cells infected with WT HIV-1 strain (IIIB) or HIV-2 (ROD) Concentration: 125, 25, 5, 1, 0.2, 0.04, 0.008 and 0.0016 μg/ml Incubation Time: 5 d Result: Exbited EC 50 value, CC 50 value and SI value of 13 nM, 26.45 μM and 2019.8 respectively against HIV-1 (IIIB). Inhibited L100I, K103N, Y181C, Y188L, E138K, F227L + V106A, and K103N + Y181C (single and double HIV mutant strains) with EC 50 s of 24, 13, 58, 760, 25, 27530 and 260 nM, respectively.
体内活性
Zlm-66 (1-5 mg/kg; i.v. and p.o. once) shows good druggability and have a good effect in vivo after oral administration [1]. 1.19 Pharmacokinetic Parameters of ZLM-66 in rat [1]. Rat IV 1 mg/kg Rat PO 5 mg/kg
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
