Customer Validation
- •Nat Commun. 2014 Oct 30;5:5352.
- •Proc Natl Acad Sci U S A. 2017 Feb 21;114(8):1922-1927.
- •Int J Radiat Oncol Biol Phys. 2016 Nov 15;96(4):867-876.
- •Antiviral Res. 2017 Mar;139:18-24.
- •Sci Rep. 2016 Oct 5;6:34652.
| Description |
Asunaprevir is a potent hepatitis C virus (HCV) NS3 protease inhibitor, with the IC50 of 0.2 nM-3.5 nM. |
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| IC50 & Target |
IC50: 0.2 nM-3.5 nM (HCV NS3 protease) |
| In Vitro |
In multiple experiments, populations of resistant colonies are markedly reduced when cells are treated with a combination of DCV and Asunaprevir[1]. Asunaprevir (ASV) inhibits the NS3 proteolytic activity of genotype 1a (H77 strain) and genotype 1b (J4L6S strain), with IC50s of 0.7 and 0.3 nM, respectively. The EC50s of ASV against replicons encoding the NS3 protease domains representing genotypes 1a, 1b, and 4a, range from 1.2 to 4.0 nM[2]. Replicon cells are maintained under selective pressure with asunaprevir at concentrations of 10 and 30 times the EC50 values (50 or 150 nM final concentrations, respectively). For genotype 1b resistance selection, replicon cells are maintained in the presence of asunaprevir at 10 or 30 times the EC50 values (30 or 90 nM final concentrations, respectively)[3]. Asunaprevir, administered at single or multiple doses of 200 to 600 mg twice daily, is generally well tolerated, achieving rapid and substantial decreases in HCV RNA levels in subjects chronically infected with genotype 1 HCV[4]. |
| In Vivo |
Asunaprevir (ASV, 3-15 mg/kg, p.o.) displays a hepatotropic disposition (liver-to-plasma ratios ranging from 40- to 359-fold across species) in several animal species. Twenty-four hours postdose, liver exposures across all species tested are ≥110-fold above the inhibitor EC50 observed with HCV genotype-1 replicons[2]. |
| References |
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| Preparing Stock Solutions |
Please refer to the solubility information to select the appropriate solvent.
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| Cell Assay
[2] |
Asunaprevir is diluted in assay buffer in 10% DMSO. Cytotoxicity is determined by incubating cells (3,000 to 10,000 cells/well) with serially diluted test compounds or DMSO for 5 days (MT-2 cells) or 4 days (all other cell types). Cell viability is quantitated using an MTS assay for MT-2 or a Cell-Titer Blue reagent assay for HEK-293, HuH-7, HepG2, and MRC5 cells, and 50% cytotoxic concentrations (CC50s) are calculated. For the HCV and BVDV replicon assays, CC50s are determined from the same wells that are later used to determine EC50s. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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| Animal Administration
[2] |
Asunaprevir is diluted in vehicle (PEG-400-ethanol, 9:1). Mice (n=9 per group; overnight fast) receive Asunaprevir (ASV) by oral gavage (5 mg/kg; vehicle of PEG-400-ethanol, 9:1). Blood samples (∼0.2 mL) are obtained by retro-orbital bleeding at 0.25, 0.5, 1, 3, 6, 8, and 24 h after dosing. Within each group, three animals are bled at 0.25, 3, and 24 h, three at 0.5 and 6 h, and three at 1 and 8 h, resulting in a composite pharmacokinetic profile. Livers and brains are also removed from mice at the terminal sampling points. Rats (n=3 per group; overnight fast) receive ASV (amorphous free acid) by oral gavage (3, 5, 10, and 15 mg/kg) in PEG-400-ethanol (9:1). Serial blood samples (∼0.3 mL) are obtained from the jugular vein predosing (0 h) and at 0.25, 0.5, 0.75, 1, 2, 4, 6, 8, 24, and 48 h postdosing. To assess tissue exposure, rats are orally administered ASV (5 or 15 mg/kg, same vehicle as above), and blood, liver, and heart samples from two rats/group are obtained at 0.17, 0.5, 1, 2, 4, 6, 8, 24, 48, and 72 h after dosing. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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| References |
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| Molecular Weight |
748.29 |
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| Formula |
C₃₅H₄₆ClN₅O₉S |
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| CAS No. |
630420-16-5 |
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| Storage |
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| Shipping | Room temperature in continental US; may vary elsewhere |
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| Solvent & Solubility |
DMSO: ≥ 42.9 mg/mL
* "<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation=""> |
Purity: 99.27%
COA (98 KB) HNMR (517 KB) LCMS (150 KB)
Handling Instructions (1252 KB)-
[1]. Pelosi LA, et al. Effect on HCV Replication by Combinations of Direct Acting Antivirals Including NS5A Inhibitor Daclatasvir. Antimicrob Agents Chemother. 2012 Jul 30.
[2]. McPhee F, et al. Preclinical Profile and Characterization of the Hepatitis C Virus NS3 Protease Inhibitor Asunaprevir (BMS-650032). Antimicrob Agents Chemother. 2012 Aug 6.
[3]. McPhee F, et al. Resistance analysis of the hepatitis C virus NS3 protease inhibitor asunaprevir.Antimicrob Agents Chemother. 2012 Jul;56(7):3670-81.
[4]. Pasquinelli C, et al. Single- and multiple-ascending-dose studies of the NS3 protease inhibitor asunaprevir in subjects with or without chronic hepatitis C. Antimicrob Agents Chemother. 2012 Apr;56(4):1838-44.
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求助各位前辈，我最近在合成的化合物水溶性很好，非常好，以至于可以随便溶解在水里，它的六氟磷酸盐也可以随意溶解在水里（大于50uM），细胞成像实验显示它根本进不去细胞，求问有没有啥方法包裹一下让它进去？我搜了一下文献，感觉多数是把脂溶性特别好的东西包裹一下弄进去的，也许是搜索姿势不对没找到我需要的答案，**点拨啊！！！
求助各位大神，现在想购买小分子数据库，求大神推荐。
我知道的免费的数据库有zinc
求推荐哪家公司或者研究所的小分子数据库可以购买，十分感谢！！！！！！
求助大家，小分子药物最新专利申请情况跟踪，之前听别人说可以在一个网站可以导出这个信息。
不知哪位大侠知道，告知一下，不胜感激！
就是蛋白质分子的小片断
是氨基酸形成的
一、首先你要明白肽是什么...........................肽是氨基酸通过酰胺键结合而成的东西.........
二、你要明白氨基酸是什么..........................氨基酸是构成蛋白质的基本单位，多种氨基酸结合为长肽链，几条长肽链再盘旋就形成了蛋白质......................
三、关于小分子肽、短肽、多肽、寡肽.......其实都是肽.......区别只是由多少个氨基酸构成而已............
所以，你的问题可以很粗暴地理解为“蛋白质对人体有没有副作用”.......
如果你营养足够的情况下，再补充这个，会导致营养过剩，从而加重身体代谢的负荷............类似就是这样子的了...........小分子肽，一般现在用于化妆品上比较多（一ye子.植物肽面膜就是这个）.......小分子肽（可以简单理解为纳米胶原蛋白），这比蛋白质（也可以粗暴理解为胶原蛋白）更加容易吸收......而用在食品上，要视乎是何种小分子肽了.....大豆肽、花生肽、大米肽....不同的肽有不同的功效.......主要可以改善风味、改善吸收、增强胃肠道功能等等.......
有机的是有机化合物的简称,它指的是含碳化合物.
但是,有四大类常见物质一般不作为有机物处理：
1、碳的氧化物,如CO和CO2.
2、碳酸及其盐,如CaCO3.
3、金属碳化物,如CaC2.
4、拟卤素及其化合物,如(CN)2与KSCN.
水的化学式为H2O,它不含有碳元素,故不是有机物.
但若所描述的水不是化学意义的水,而是自然界存在的天然水,那么,水中会溶有一定量的有机物.
