| Description | Reverse transcriptase-IN-1 is a diarylbenzopyrimidine (DABP) analogue and a potent inhibitor of HIV-1 nonnucleoside reverse transcriptase with an IC50of 13.7 nM. |
| In vitro | Reverse transcriptase-IN-1 对HIV-1 IIIB、E138K和K103N突变体表现出抗病毒活性，相应的EC50值分别为3.4 nM、4.3 nM和3.6 nM[1]。 |
| In vivo | Reverse transcriptase-IN-1 的药代动力学研究和安全性评估表明，其具有平均滞留时间（MRTs）分别为11.8小时（5 mg/kg，经口）和11.4小时（1 mg/kg，静脉注射）。在5 mg/kg剂量下，Reverse transcriptase-IN-1 的最大血药浓度（Cmax）达到39.9 ng/mL。同一剂量下，Reverse transcriptase-IN-1 的口服生物利用度显著提高到16.5%。大鼠体内Reverse transcriptase-IN-1 的本征微粒体清除率为33.2 μL/min/mg蛋白[1]。 |
| Target activity | HIV-1 RT:13.7 nM |
| molecular weight | 447.45 |
| Molecular formula | C25H17N7O2 |
| CAS | 2380001-43-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 12 mg/mL (26.82 mM), Sonication and heating to 60℃ are recommended. |
| References | 1. Han S, et al. Molecular Hybridization-Inspired Optimization of Diarylbenzopyrimidines as HIV-1 Nonnucleoside Reverse Transcriptase Inhibitors with Improved Activity against K103N and E138K Mutants and Pharmacokinetic Profiles. ACS Infect Dis. 2019 Oct 24. |