依伐卡托|T2588|TargetMol

Ivacaftor
873054-44-5

￥197 1mg 起订

￥413 5mg 起订

￥619 10mg 起订

上海更新日期：2024-12-02

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产品详情:

中文名称：: 依伐卡托

英文名称：: Ivacaftor

CAS号：: 873054-44-5

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.98%

产品类别：: 抑制剂

货号：: T2588

Product Introduction

Bioactivity

名称	Ivacaftor
描述	Ivacaftor (VX-770) (VX-770) is a potentiator of CFTR targeting G551D-CFTR (EC50: 100 nM) and F508del-CFTR (EC50: 25 nM) in Fisher rat thyroid cells, respectively.
细胞实验	HEK293 cells were seeded on poly-lysine precoated six-well plates at a density of 1.3 x 10^6 cells/well. Six hours after seeding, cells were transiently transfected with 1μg of ABCB4-encoding plasmids using Turbofect, following the manufacturer's instructions. Twenty-four hours post-transfection, cells were washed twice with HBSS, then the medium was replaced by phenol red-free DMEM containing 0.5 mmol/L sodium taurocholate and 0.02% fatty acid–free bovine serum albumin (BSA) in the presence or absence of 10 μmol/L of ivacaftor, 50 μM/L of UDCA, and 10 μmol/L of ivacaftor plus 50 μM/L of UDCA. Media were collected after 24 hours [2].
动物实验	Male mouse,Sprague?Dawley rats,beagle dog,and cynomolgus monkeys (n = 3/group) were administered a single iv dose of compound formulated in dimethyl isosorbide/ethanol/PEG400/5% dextrose in water (D5W) (10%/15%/35%/40%) at the nominal dose indicated in a dose volume of 1 mL/kg.Blood samples (0.3 mL,sodium heparin anticoagulant) were collected from an indwelling carotid cannula at the following nominal time points: at predose,5,15,30,and 45 min and 1,2,4,6,8,12,24,36,and 48 h following iv administration and at predose,0.25,0.50,1,1.5,2,4,8,12,and 24 h following oral administration.The concentration of compound in the plasma samples was determined with a liquid chromatography/tandem mass spectrometry (LC/MS/MS) method,which had a lowest limit of quantitation (LLOQ) of 1 ng/mL and a linearity range between 1 and 2500 ng/mL [3].
体外活性	VX-770将温度修正的F508del-FRT细胞中，通过forskolin刺激的IT增加约6倍，其EC50为25 ± 5 nM。在加入VX-770之前，CFTR通道已经暴露于PKA（75 nM）和ATP（1 mM）的最大有效浓度下。在这些条件下，10 μM VX-770将G551D CFTR的Po增加了约6倍[1]。暂时表达ABCB4-wt或突变体的HEK293细胞，被10 μmol/L的ivacaftor（VX-770）处理24小时。ivacaftor处理使ABCB4-G535D的PC分泌活性增加3倍，ABCB4-G536R增加13.7倍，ABCB4-S1076C增加6.7倍，ABCB4-S1176L增加9.4倍，以及ABCB4-G1178S增加5.7倍[2]。
体内活性	在大鼠剂量比例性研究中，通过口服悬浮剂型给药，Ivacaftor的剂量从1到200 mg/kg（中间剂量为3, 10, 30和100）时，其AUC和Cmax呈线性增加。在比格犬中，口服剂量从3到80 mg/kg（中间剂量为10, 30和60）增加时，观察到类似趋势，证实了高水平的口服吸收。通过从四种物种的异速生长估计，预测人类对Ivacaftor的肝脏清除率为4.7 mL min1 kg1，约占肝血流量的23% [3]。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 55 mg/mL (140.13 mM)
关键字	Cystic fibrosis transmembrane conductance regulator \| Ivacaftor \| inhibit \| CFTR \| VX 770 \| Autophagy \| Inhibitor \| VX770
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相关库	经典已知活性库 \| 已知活性化合物库 \| EMA 上市药物库 \| FDA 上市药物库 \| 离子通道库 \| 药物功能重定位化合物库 \| 抗癌临床化合物库

依伐卡托|||VX-770|||Ivacaftor (VX-770)|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子