Lumacaftor | CFTR corrector, DUSP18 inhibitor | Probechem Biochemicals

Chemical Structure : Lumacaftor

CAS No.: 936727-05-8

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Lumacaftor (VX-809, VRT 826809, VX809)

货号: PC-43442Not For Human Use, Lab Use Only.

VX-809 (Lumacaftor, VRT 826809) is a potent CFTR corrector that increases F508del-CFTR-mediated chloride transport amd improves F508del-CFTR maturation in FRT cells with EC50 of 0.1 and 0.5 uM, respectively, also inhibits dual specificity phosphatase 18 (DUSP18).

规格	价格	库存
10 mg	￥880	In stock
50 mg	￥1580	In stock
100 mg	￥2180	In stock
250 mg		Get quote
1 g		Get quote

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生物&药学活性

VX-809 (Lumacaftor, VRT 826809) is a potent CFTR corrector that increases F508del-CFTR-mediated chloride transport amd improves F508del-CFTR maturation in FRT cells with EC50 of 0.1 and 0.5 uM, respectively, also inhibits dual specificity phosphatase 18 (DUSP18).
VX-809 (Lumacaftor, VRT 826809) improves F508del-CFTR processing in the endoplasmic reticulum and enhances chloride secretion to approximately 14% of non-CF human bronchial epithelial cells (EC50=81 nM).
VX-809 (Lumacaftor, VRT 826809) exhibits biochemical and functional characteristics similar to normal CFTR, including biochemical susceptibility to proteolysis, residence time in the plasma membrane, and single-channel open probability after F508del-CFTR corrected by VX-809.
VX-809 (Lumacaftor, VRT 826809) inhibits CRC growth in mice and synergistically enhances anti-tumor immunity when combined with an anti-PD-1 antibody.

物理化学性质&存储条件

分子量	452.41
分子式	C24H18F2N2O5
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Benzoic acid, 3-[6-[[[1-(2,2-difluoro-1,3-benzodioxol-5-yl)cyclopropyl]carbonyl]amino]-3-methyl-2-pyridinyl]-

参考文献

1. Van Goor F, et al. Proc Natl Acad Sci U S A. 2011 Nov 15;108(46):18843-8.

2. Okiyoneda T, et al. Nat Chem Biol. 2013 Jul;9(7):444-54.

3. Farinha CM, et al. Chem Biol. 2013 Jul 25;20(7):943-55.

4. Kopeikin Z, et al. J Cyst Fibros. 2014 Sep;13(5):508-14.

Lumacaftor (VX-809, VRT 826809, VX809)

生物&药学活性

物理化学性质&存储条件

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Lumacaftor (VX-809, VRT 826809, VX809)

生物&药学活性

物理化学性质&存储条件

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