中文名称: | Aprepitant 促销 | ||||
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英文名称: | Aprepitant | ||||
别名: | 阿瑞匹;5-[2(R)-[1(R)-[3,5-二(三氟甲基)苯基]乙氧基]-3(S)-(4-氟苯基)吗啉-4-基甲基]-3,4-二氢-2H-1,2,4-三唑-3-酮 5-(((2R,3S)-2-((R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)morpholino)methyl)-1H-1,2,4-triazol-3(2H)-one | ||||
CAS No: | 170729-80-3 | 分子式: | C23H21F7N4O3 | 分子量: | 534.43 |
CAS No: | 170729-80-3 | ||||
分子式: | C23H21F7N4O3 | ||||
分子量: | 534.43 | ||||
MDL: | MFCD12912491 |
基本信息
产品编号: |
A10953 |
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产品名称: |
Aprepitant |
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CAS: |
170729-80-3 |
储存条件 |
粉末 |
-20℃ |
四年 |
分子式: |
溶于液体 |
-80℃ |
6个月 |
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分子量: |
534.43 |
-20℃ |
1个月 |
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化学名: |
5-(((2R,3S)-2-((R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)morpholino)methyl)-1H-1,2,4-triazol-3(2H)-one |
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Solubility (25°C): |
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体外:
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DMSO |
107mg/mL (200.21mM) |
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Ethanol |
25mg/mL (46.77mM) |
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Water |
Insoluble |
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体内(现配现用): |
5% DMSO+corn oil |
13mg/mL |
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<1mg/ml表示微溶或不溶。 |
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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。 |
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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 |
1.8712mL |
9.3558mL |
18.7115mL |
5mM |
0.3742mL |
1.8712mL |
3.7423mL |
10mM |
0.1871mL |
0.9356mL |
1.8712mL |
50mM |
0.0374mL |
0.1871mL |
0.3742mL |
生物活性
产品描述 |
一种选择性的高亲和力的神经激肽1受体拮抗剂,Kd值为86pM。 |
靶点 |
Kd:86pM (Neurokinin 1 receptor) |
体外研究 |
Aprepitant decreases the metabolic activity with an estimated IC50 value of 20µM.Aprepitant induces cell-growth inhibition and G1 cell-cycle arrest.Aprepitant significantly induces apoptosis in Nalm-6 cells,and the apoptosis is mediated through caspase-3 activation.Aprepitant (20µM) induces p53 accumulation and expression of pro-apoptotic p53 target genes.Aprepitant (1,5,10µM) inhibits HIV infection in MDM from both depressed and not depressed HIV negative individuals ex vivo in a dose-dependent manner.IC90 value of aprepitant is equivalent to 10μM,and the IC50 value is about 5μM. |
体内研究 |
Aprepitant prevents the increase of NK-1R expression induced by in vivo NHP infection with B.burgdorferi.Aprepitant treatment prevents B.burgdorferi-induced increases in CCL2 protein levels in the CSF of NHPs.Aprepitant treatment prevents B.burgdorferi-induced increases in CCL2 and CXCL13 mRNA expression in the dorsal root ganglia of NHPs,prevents B.burgdorferi-induced increases in CCL2,CXCL13,IL-17A,and IL-6 mRNA expression in the spinal cord of NHPs.Aprepitant treatment attenuates B.burgdorferi infection-induced reductions in astrocyte activity/numbers.Aprepitant (10mg/kg,i.p.) significantly attenuates the CPP expression and locomotor activation produced by AMPH and cocaine in mice.In contrast,aprepitant significantly enhances the expression of CPP produced by morphine while significantly suppressing the locomotor activity of the mice conditioned with morphine.Aprepitant does not induce significant CPP or conditioned place aversion or locomotor activation or suppression.Aprepitant (125mg/day,p.o.) results in 1 log reduction in plasma levels of viral RNA as compared to non-treated controls. |
推荐实验方法(仅供参考)
细胞实验: |
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The inhibitory effect of aprepitant on metabolic activity of Nalm-6 cells is assessed by uptake of thiazolyl blue tetrazolium bromide (MTT) by viable cells.Cells are plated onto 96-well plates at a density of 5000 cells/well.After treatment with aprepitant at 5,10,15,20 and 30µM for 24,36 and 48h,the cells are further incubated with 100μL of MTT (0.5mg/mL) at 37℃ for 3h.Untreated cells are defined as the control group.Following solubilization of precipitated formazan with 100μL of DMSO,the optical densitometry is measured with an ELISA reader at a wavelength of 578nm. |
动物实验: |
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Fifteen rhesus macaques are anesthetized and inoculated intrathecally with 1×108 live spirochetes into the cisterna magna,whereas five rhesus macaques are left uninfected and receive 1mL of RPMI 1640 medium after removing an equivalent volume of CSF.The establishment of in vivo B.burgdorferi infection is confirmed by positive culture from at least necropsy tissue sample.The first set of animals are studied for 2 weeks and included two control animals (one of which is treated with aprepitant),two infected and untreated animals,and two infected animals that are treated with aprepitant.The second set of animals are studied for 4 weeks and included three control animals (one of which is treated with aprepitant),five infected and untreated animals,and four infected animals treated with aprepitant.Animals receive an average dose of aprepitant of 28±6mg/kg per day p.o.daily,and drug treatments are started 2 days before inoculation.These doses are consistent with standard veterinary regimens for the chosen drugs in NHP,and the 4-week duration of the study precludes the development of neural pathology that occurs at 8 weeks following B.burgdorferi infection. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )