Product IntroductionBioactivity英文名:
Maraviroc描述: Maraviroc (Selzentry) 是一种 C-C 趋化因子受体 5 拮抗剂,具有抑制HIV 的活性。
细胞实验: 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)
激酶实验: Inhibition of chemokine binding to CCR5: Binding of 125I-labeled MIP-1α, MIP-1β, and RANTES to CCR5 is measured using intact HEK-293 cells stably expressing the receptor or membrane preparations thereof. Briefly, cells are resuspended in binding buffer (50 mM HEPES containing 1 mM CaCl2, 5 mM MgCl2, and 0.5% bovine serum albumin [BSA] and adjusted to pH 7.4) to a density of 2 × 106 cells/ml. For membrane preparations, phosphate-buffered saline (PBS)-washed cells are resuspended in lysis buffer (20 mM HEPES, 1 mM CaCl2, 1 tablet COMPLETE per 50 mL, pH 7.4) prior to homogenization in a Polytron hand-held homogenizer, ultracentrifugation (40,000× g for 30 min), and resuspension in binding buffer to a protein concentration of 0.25 mg/mL (12.5 μg of membrane protein is used in each well of a 96-well plate). 125I-radiolabeled MIP-1α, MIP-1β, and RANTES are prepared and diluted in binding buffer to a final concentration of 400 pM in the assay. Maraviroc dilutions are added to each well to a final volume of 100 μL, the assay plates incubate for 1 hour, and the contents filter through preblocked and washed Unifilter plates which are counted following overnight drying.
体外活性: 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.
体内活性: 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。
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 55 mg/mL (107.07 mM)
Ethanol : 51.4 mg/mL (100 mM)
关键字:
Maraviroc |
CC chemokine receptor |
UK427857 |
inhibit |
Human immunodeficiency virus |
HIV |
CCR |
Inhibitor |
UK 427857相关产品:
4-Chloro-2-(trifluoroacetyl)aniline hydrochloride |
Bellidifolin |
TAK-220 |
L-Cycloserine |
Aprepitant |
Mk-6186 HCl |
PKF050-638 |
Cys-TAT(47-57) acetate(583836-55-9 Free base) |
Benzalphthalide |
Ganoderic acid B相关库:
FDA-Approved Drug Library |
Drug Repurposing Compound Library |
Anti-Neurodegenerative Disease Compound Library |
Anti-COVID-19 Compound Library |
Membrane Protein-targeted Compound Library |
Bioactive Compounds Library Max |
Human Metabolite Library |
Inhibitor Library |
EMA Approved Drug Library |
Orally Active Compound Library