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抑制剂/激活剂

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凋亡与自噬

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Ivacaftor 依伐卡托; VX-770

Ivacaftor (VX-770)是一种CFTR的选择性增强剂，靶向作用于G551D-CFTR和F508del-CFTR，在fisher大鼠甲状腺细胞中EC50分别为100 nM和25 nM。

货号：
TK0208
规格：

1mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	873054-44-5
生物活性	Ivacaftor (VX-770) is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively.
分子式	C24H28N2O3
分子量	392.49
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶解性数据	DMSO : 50 mg/mL (127.39 mM; Need ultrasonic)
体内研究	Ivacaftor (1-200 mg/kg, p.o.) exhibits good oral bioavailability in rat.
体外研究	Ivacaftor (10 µM) increases the PC secretion activity by 3-fold for ABCB4-G535D, 13.7-fold for ABCB4-G536R, 6.7-fold for ABCB4-S1076C, 9.4-fold for ABCB4-S1176L, and 5.7-fold for ABCB4-G1178S. Ivacaftor corrects the functional defect of ABCB4 mutants. Ivacaftor (10 μM) significantly increases CFTR activity in W1282X-expressing cells compared to R1162X CFTR cells. Ivacaftor shows no significant activity against 160 targets tested including the GABAA benzodiazepine receptor. Ivacaftor increases the chloride secretion with an EC50 of 0.236 ± 0.200 μM, a 10-fold shift in potency compared to the F508del HBEs. In recombinant cells, VX-770 increases CFTR channel open probability (Po) in both the F508del processing mutation and the G551D gating mutation. VX-770 increases forskolin-stimulated IT in temperature-corrected F508del-FRT cells by appr 6-fold with an EC50 of 25 nM.
文献	•Front Cell Dev Biol. 2021 May 11;9:678209. •Org Process Res Dev. 2019, 23, 11, 2302-2322.
纯度及产品资料	98%

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