| Description | Maraviroc (Selzentry) is a C-C Chemokine Receptor Type 5 (CCR5) antagonist, and for MIP-1α(IC50=3.3 nM), MIP-1β (IC50=7.2 nM) and RANTES(IC50=5.2 nM).Maraviroc inhibits HIV-1 entry via CCR5 coreceptor interaction. |
| In vitro | 在犬类中,口服2 mg/kg Maraviroc,1.5小时后达到峰浓度为256 ng/ml,生物有效性为40%.在大鼠中,Maraviroc半衰期为0.9小时,大约30%给药剂量从肠道吸收.雌性RAG-hu小鼠实验显示,Maraviroc完全保护小鼠免受HIV-1感染. |
| In vivo | 在MIP-1β, MIP-1α和RANTES中,Maraviroc(IC50=7-30 nM)抑制趋化因子诱导的细胞内钙重新分配的下游。 |
| Cell experiments | Drug susceptibility assays are performed in 24-well tissue culture plates. Duplicate eight-point dilution series of Maraviroc are prepared in DMSO and medium to yield a final DMSO concentration of 0.1% (vol/vol) in the assay. PHA-stimulated PBMC or PM-1 cells are infected with virus for 1 hour at 37 °C. Cells are subsequently washed once, and 3.6 × 105 PBMC or 2.0 × 105 PM-1 cells are added to each well of assay plates containing diluted Maraviroc. Plates are incubated for 5 days (lab-adapted strains) or 7 days (primary isolates) at 37 °C in a humidified 5% CO2 (vol/vol) atmosphere.(Only for Reference) |
| Target activity | MIP-1α:3.3 nM, RANTES:5.2 nM, MIP-1β:7.2 nM |
| Synonyms | Celsentri, 马拉维若, UK-427857, Selzentry |
| molecular weight | 513.67 |
| Molecular formula | C29H41F2N5O |
| CAS | 376348-65-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 55 mg/mL (107.07 mM) Ethanol: 51.4 mg/mL (100 mM) |
| References | 1. Dorr P, et al. Antimicrob Agents Chemother. 2005, 49(11), 4721-4732. 2. Neff CP, et al. PLoS One. 2011, 6(6), e20209. 3. Tan S, Li J Q, Cheng H, et al. The anti-parasitic drug suramin potently inhibits formation of seminal amyloid fibrils and their interaction with HIV-1[J]. Journal of Biological Chemistry. 2019: jbc. RA118. 006797. 4. Yang J Y, Zhang J, Lu R, et al. T cell–derived exosomes induced macrophage inflammatory protein‐1α/β drive the trafficking of CD8+ T cells in oral lichen planus[J]. Journal of cellular and molecular medicine. 2020 |
| Citations | 1. Yang J Y, Zhang J, Lu R, et al. T cell–derived exosomes induced macrophage inflammatory protein‐1α/β drive the trafficking of CD8+ T cells in oral lichen planus. Journal of Cellular and Molecular Medicine. 2020 2. Tan S, Li J Q, Cheng H, et al. The anti-parasitic drug suramin potently inhibits formation of seminal amyloid fibrils and their interaction with HIV-1. Journal of Biological Chemistry. 2019: jbc. RA118. 006797 3. Wu Q, Cui L, Ma W, et al.A novel small-molecular CCR5 antagonist promotes neural repair after stroke.Acta Pharmacologica Sinica.2023: 1-13. 4. Horie M, Takagane K, Itoh G, et al.Exosomes secreted by ST3GAL5 high cancer cells promote peritoneal dissemination by establishing a pre‐metastatic microenvironment.Molecular Oncology.2023 |