| 名稱 | Maraviroc |
| 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. |
| 細(xì)胞實(shí)驗(yàn) | 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) |
| 激酶實(shí)驗(yàn) | 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. |
| 體外活性 | 在MIP-1β, MIP-1α和RANTES中,Maraviroc(IC50=7-30 nM)抑制趨化因子誘導(dǎo)的細(xì)胞內(nèi)鈣重新分配的下游。 |
| 體內(nèi)活性 | 在犬類(lèi)中,口服2 mg/kg Maraviroc,1.5小時(shí)后達(dá)到峰濃度為256 ng/ml,生物有效性為40%.在大鼠中,Maraviroc半衰期為0.9小時(shí),大約30%給藥劑量從腸道吸收.雌性RAG-hu小鼠實(shí)驗(yàn)顯示,Maraviroc完全保護(hù)小鼠免受HIV-1感染. |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 55 mg/mL (107.07 mM), Sonication is recommended.
Ethanol : 51.4 mg/mL (100.06 mM), Sonication is recommended.
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| 關(guān)鍵字 | UK427857 | UK 427857 | RANTES | MIP-1β | MIP-1α | Maraviroc | Inhibitor | inhibit | Human immunodeficiency virus | HIVProtease | HIV Protease | HIV | CCR | CC chemokine receptor |
| 相關(guān)產(chǎn)品 | Tenofovir | Valproic Acid | Chloroquine phosphate | Emtricitabine | Dolutegravir intermediate-1 | Dextran sulfate sodium salt (MW 5000) | Lamivudine | 5-Fluorouracil | Decanedioic acid | Stavudine | Kaempferol | Dimethyl fumarate |
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