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Maraviroc 促销  ≥98%(HPLC)

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包装规格：5mg 25mg 100mg in glass bottle
溶解性：溶于DMSO(100mg/ml)和乙醇
产品描述：基本信息 产品编号： M10083 产品名称： Maraviroc（UK-427857） CAS: 376348-65-1   储存条件 粉末 -20℃ 四年     分子式： C29H41F2N5O 溶于液体 -80℃ 6个月 分子量： 513.67 -20℃ 1个月 化学名：  4,4-Difluoro-N-[(1S)-3-[(3-exo)-3-[3-methyl-5-(1-methylethyl)-4H-1,2,4-triazol-4-yl]-8-azabicyclo[3.2.1]oct-8-yl]-1-phenylpropyl]cyclohexanecarboxamide Solubility (25°C)：   体外:   DMSO 100mg/mL (194.67mM) Ethanol 100mg/mL (194.67mM) Water Insoluble 体内(现配现用): 2% DMSO+corn oil 10mg/mL ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 1.9468mL 9.7339mL 19.4678mL 5mM 0.3894mL 1.9468mL 3.8936mL 10mM 0.1947mL 0.9734mL 1.9468mL 50mM 0.0389mL 0.1947mL 0.3894mL   生物活性 产品描述 一种CKR5受体拮抗剂，IC50：6.4nM。 靶点 CCR5 (Cell-free assay) MIP-1α(Cell-free assay) RANTES(Cell-free assay) MIP-1β(Cell-free assay)   3.30nM 5.2nM 7.2nM   体外研究 Maraviroc (UK-427857) is a selective CCR5 antagonist with potent anti-human immunodeficiency virus type 1 (HIV-1) activity.Maraviroc inhibits the downstream event of chemokine-induced intracellular calcium redistribution,with IC50s ranging from 7 to 30nM obtained against MIP-1β,MIP-1α and RANTES.Maraviroc (UK-427857) is active (IC90) at low nanomolar concentrations against HIV-1 Ba-L (a lab-adapted R5 strain) when measured in a 5-day antiviral assay using either isolated multiple (pooled) donor PBMC (IC90,3.1nM),single-donor PBMC (IC90,1.8nM) or PM-1 cells (IC90,1.1nM). 体内研究 Clearance values are moderate to high in both rat and dog species following i.v.administration (74 and 21mL/min/kg,respectively).Maraviroc also has a moderate volume of distribution in both species (4.3 to 6.5 liters/kg).The half-life values of maraviroc are 0.9h in the rat and 2.3h in the dog.Following oral administration (2mg/kg) to the dog,the Cmax(256ng/mL) occurs 1.5h.post-dose,and the bioavailability is 40%.For the rat,investigation of the concentrations obtain in the portal vein following oral administration indicated that approximately 30% of the administered dose is absorbed from the intestinal tract.In the DSS/TNBS colitis and in the transfer model,Maraviroc attenuates development of intestinal inflammation by selectively reducing the recruitment of CCR5 bearing leukocytes.   推荐实验方法(仅供参考) 激酶实验： Binding of 125I-labeled MIP-1α,MIP-1β,and RANTES to CCR5 is measured essentially using intact HEK-293 cells stably expressing the receptor or membrane preparations thereof.Briefly,cells are resuspended in binding buffer (50mM HEPES containing 1mM CaCl2,5mM 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 (20mM HEPES,1mM CaCl2,1 tablet COMPLETE per 50mL,pH 7.4;Boehringer) 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 0.25mg/mL (12.5μg 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 400pM in the assay.Appropriate maraviroc dilutions are added to each well to a final volume of 100μL,the assay plates incubated for 1h,and the contents filtered through preblocked and washed Unifilter plates which are counted following overnight drying.   细胞实验:   HEK-293 cell aliquots (100μL at 1×106 cells/mL) are plated into poly-D-lysine-coated plates and incubated at 37℃ overnight.A 1:1 mix of soluble recombinant human CD4 (sCD4) (diluted to 4.5nM in culture medium) and HIV-1 gp120 is incubated at room temperature for 15 min prior to its addition to PBS-washed cells in the presence of dilutions of maraviroc to enable IC50 determination.The assay plates are incubated at 37℃ for 1h and washed.Eu3+-labeled anti-gp120 antibody (1/500 dilution in assay buffer) is added to each well (50μL) and incubated for 1h.The plate is washed three times with wash buffer prior to the addition of enhancement solution (200μL/well) and measurement of Eu3+ fluorescence (Victor2multilabel counter;“Europium”protocol).Nonspecific binding is taken as the fluorescence measured for gp120 incubated with cells in the absence of preincubation with sCD4.   动物实验:   Rats and Dogs Preclinical pharmacokinetic studies are carried out with maraviroc following a single intravenous and oral administration to both male Sprague-Dawley rats (1mg/kg of body weight given intravenously [i.v.] and 10mg/kg given orally [p.o.];n=2) and male beagle dogs (0.5mg/kg i.v.and 2mg/kg p.o;n=4).Plasma samples are taken for up to 24h postdose,and the concentrations of unchanged maraviroc are determined using a specific high-performance liquid chromatography-tandem mass spectrum assay. Mice Splenocytes are collected from 6-10 week old CCR5-/-mice or wild-type controlmice (n=8 per group) and naive CD4+CD45RB high T-cells are isolated by cell sorting. A total of 3×105 CD45RBhigh cells are then injected intravenously into Rag1-/-mice that are subsequently weighed and assessed for fecal score every 20 days to evaluate IBD development.To investigate whether Maraviroc rescues from intestinal inflammation induced by transfer colitis,Rag1-/-mice are injected with CD4+CD45RB-/-T-cells and 34 days later randomized into either a control group (no further treatment,n=6) or treatment with Maraviroc,50mg/kg/d Maraviroc per os (n=4) for 3 weeks,5 d/week.
保存条件：-20℃

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