| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| I407897-1ml |
1ml |
现货  |
|
| 别名 | 依伐卡托 (VX-770) |
|---|---|
| 英文别名 | N-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Ivacaftor (VX-770) |
| 生化机理 | Ivacaftor（VX-770）是一种针对 G551D-CFTR 和 F508del-CFTR 的 CFTR 选择性增效剂，在渔鼠甲状腺细胞中的 EC50 分别为 100 nM 和 25 nM。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 激活剂 |
| 作用机制 | CFTR 激活剂 |
| 产品介绍 |
Ivacaftor (VX-770)是一种囊性纤维化跨膜传导调节器(CFTR)的增强剂，靶向作用于G551D-CFTR和F508del-CFTR，EC50分别为100 nM和25 nM。Is a CFTR activator Information Ivacaftor (VX-770) Ivacaftor (VX-770) is a selective potentiator of CFTR targeting G551D-CFTR and F508del-CFTR with EC50 of 100 nM and 25 nM in fisher rat thyroid cells, respectively. Ivacaftor (10 μM) significantly increases the forskolin-stimulated Cl- secretion (IT) by ~4-fold with an EC50 of 100 nM in the recombinant Fisher rat thyroid (FRT) cells expressing G551D gating mutation of CFTR, and by ~6-fold with an EC50 of 25 nM in the recombinant cells expressing temperature-corrected F508del processing mutation of CFTR. Consistent with the increases in the forskolin-stimulated IT, Ivacaftor (10 μM) increases the open probability (Po) of G551D-, F508del-, and wild-type CFTR by ~6-fold, ~5-fold and ~2-fold, respectively, indicating that Ivacaftor acts directly on CFTR to increase its gating activity. In primary cultured human CF bronchial epithelia (HBE) carrying the G551D and F508del CFTR mutations, Ivacaftor (10 μM) potently increases the forskolin-stimulated IT by ~10-fold from 5% to a maximum level of 48% of that measured in non-CF HBE, with an EC50 of 236 nM displaying ~70-fold more potency compared with the commonly used CFTR potentiator genistein, which has an EC50 of 16 μM. In HBE with F508del homozygous CFTR, Ivacaftor causes a significant increase in the forskolin-stimulated IT with an EC50 of 22 nM, to a less extent from 4% to 16% of non-CF HBE compared with the effect in G551D/F508del HBE. Due to CFTR potentiation, Ivacaftor inhibits excessive ENaC-mediated Na+ and fluid absorption with an IC50 of 43 nM, and decreases the amiloride response, resulting in an increase in the surface fluid and cilia beat frequency (CBF) in G551D/F508del HBE. In vivo
cell lines： Concentrations： Incubation Time： Powder Purity:≥99% |
| ALogP | 4.516 |
|---|---|
| hba_count | 2 |
| HBD Count | 3 |
| Rotatable Bond | 4 |
| Canonical SMILES | CC(C)(C)C1=CC(=C(NC(=O)C2=CNC3=C(C=CC=C3)C2=O)C=C1O)C(C)(C)C |
|---|---|
| 分子量 | 392.49 |
| Reaxy-Rn | 11821038 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11821038&ln= |
| DMSO(mg / mL) Max Solubility | 78 |
|---|---|
| DMSO(mM) Max Solubility | 198.73 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 11821038 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11821038&ln= |
| Concentration(Compounding value) | 9-11(mmol/L) |
|---|---|
| Record the entire process by video | Conform |
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