| Description | Pirmitegravir (STP0404) is a potent and selective inhibitor of allosteric integrase (ALLINI) targeting the LEDGF/p75 binding site. Pirmitegravir inhibits PBMC. Pirmitegravir inhibits PBMC.Pirmitegravir has significant antiviral activity and may be useful in the study of HIV virus infection. |
| In vitro | 在 CEMx174 细胞中，Pirmitegravir 的 IC50 为 1.4 nM，抑制双向 HIV-189.6[1]。Pirmitegravir 是一种高效的 ALLINI，同时抑制野生型和 Ral 耐药 HIV-1 菌株，IC50 值范围从皮摩尔到个位数纳摩尔[1]。Pirmitegravir 对 HIV-1NL4-3 的 IC50 为 0.41 nM 在 10 μM (TC50 >10μM) 浓度下，在人 PBMC 中没有表现出可观察到的细胞毒性[1]。 |
| In vivo | 对于每日一次给药，Pirmitegravir 表现出适当的 PK 特征[1]。 大鼠（500、1000 和 2000 mg/kg/天）缺乏微核诱导和骨髓细胞增殖抑制潜力的表现，支持 Pirmitegravir 不具有基因毒性的结论[1]。 Pirmitegravir 已在大鼠和狗中进行了研究[1]。 |
| Target activity | CEMx174 cells:1.4 nM, HIV-1:0.41 nM |
| Synonyms | STP0404 |
| molecular weight | 495.01 |
| Molecular formula | C27H31ClN4O3 |
| CAS | 2245231-10-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 55 mg/mL (111.11 mM) |
| References | 1. Maehigashi T, et al. A highly potent and safe pyrrolopyridine-based allosteric HIV-1 integrase inhibitor targeting host LEDGF/p75-integrase interaction site. PLoS Pathog. 2021;17(7):e1009671. 2. Singer MR, et al. The Drug-Induced Interface That Drives HIV-1 Integrase Hypermultimerization and Loss of Function. mBio. 2023 Feb 28;14(1):e0356022. 3. Dinh T, et al. The structural and mechanistic bases for the viral resistance to allosteric HIV-1 integrase inhibitor pirmitegravir. bioRxiv [Preprint]. 2024 Jan 26:2024.01.26.577387. |