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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Membrane Transporter & Ion Channel > IvacaftorCAS：873054-44-5
Molecular Formula：C24H28N2O3
Molecular Weight：392.49
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 873054-44-5 |
| Name | Ivacaftor |
| Molecular Formula | C24H28N2O3 |
| Molecular Weight | 392.49 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD17171361 |
| SMILES | CC(C)(C1=C(C=C(C(C(C)(C)C)=C1)O)NC(C2=CNC3=C(C2=O)C=CC=C3)=O)C |
| Target Point | CFTR |
| Passage | Membrane Transporter&Ion Channel |
| Background | Ivacaftor is a potent CFTR synergist. |
| Biological Activity | Ivacaftor是一种有效的 CFTR 增效剂，靶向G551D-CFTR和F508del-CFTR的EC50分别为100 nM 和 25 nM。[1-4] |
| In Vitro | Ivacaftor(10μM)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，ABCB4增加5.7倍 - G1178S。 Ivacaftor纠正了ABCB4突变体的功能缺陷[1]。与R1162X CFTR细胞相比，Ivacaftor(10μM)显著增加表达W1282X的细胞中的CFTR活性[2]。 Ivacaftor显示对160个测试目标没有显著活性，包括GABAA苯二氮卓受体。 Ivacaftor增加氯离子分泌，EC50为0.236±0.200μM，与F508del HBE相比效力变化10倍[3]。在重组细胞中，VX-770增加F508del加工突变和G551D门控突变中的CFTR通道开放概率(Po)。 VX-770可将温度校正的F508del-FRT细胞中毛喉素刺激的IT增加6倍，EC50为25 nM [4]。 |
| In Vivo | Ivacaftor(1-200 mg/kg，po)在大鼠中表现出良好的口服生物利用度[3]。 |
| Data Literature Source | [1]. Delaunay JL，et al. Functional defect of variants in the adenosine triphosphate-binding sites of ABCB4 and their rescue by the cystic fibrosis transmembrane conductance regulator potentiator，ivacaftor (VX-770). Hepatology. 2017 Feb;65(2):560-570 [2]. Mutyam V，et al. Therapeutic benefit observed with the CFTR potentiator，ivacaftor，in a CF patient homozygous for the W1282X CFTR nonsense mutation. J Cyst Fibros. 2017 Jan;16(1):24-29 [3]. Hadida S，et al. Discovery of N-(2，4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1，4-dihydroquinoline-3-carboxamide (VX-770，ivacaftor)，a potent and orally bioavailable CFTR potentiator. J Med Chem. 2014 Dec 11;57(23):9776-9 [4]. Van Goor F，et al. Rescue of CF airway epithelial cell function in vitro by a CFTR potentiator，VX-770. Proc Natl Acad Sci U S A. 2009 Nov 3;106(44):18825-30. |
| Unit | Bottle |
| Specification | 10mg 50mg |
是一种有效的 CFTR 增效剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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