购物车
- 全部删除
- 您的购物车当前为空
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。
为众多的药物研发团队赋能,
让新药发现更简单!
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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
2 mg | ¥ 283 | 现货 | |
5 mg | ¥ 429 | 现货 | |
10 mg | ¥ 722 | 现货 | |
25 mg | ¥ 1,470 | 现货 | |
50 mg | ¥ 2,730 | 现货 | |
100 mg | ¥ 3,970 | 现货 | |
200 mg | ¥ 5,790 | 现货 | |
500 mg | ¥ 8,870 | 期货 | |
1 mL x 10 mM (in DMSO) | ¥ 515 | 现货 |
产品描述 | 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. |
靶点活性 | MIP-1β:7.2 nM, MIP-1α:3.3 nM, RANTES:5.2 nM |
体外活性 | 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。 |
体内活性 | 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. |
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. |
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) |
别名 | 马拉维若, Celsentri, UK-427857, Selzentry |
分子量 | 513.67 |
分子式 | C29H41F2N5O |
CAS No. | 376348-65-1 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 55 mg/mL (107.07 mM) Ethanol: 51.4 mg/mL (100 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
|
版权所有©2015-2024 TargetMol Chemicals Inc.保留所有权利.