VX-809 (Lumacaftor)

Catalog No. A10986

VX-809 (Lumacaftor)是用于治疗囊性纤维化（CF）的第二种口服研究候选化合物，通过促进突变型CFTR(F508del-CFTR)的成熟，从而纠正囊性纤维症中常见的CFTR突变，在fisher大鼠甲状腺细胞中EC50为0.1 μM。

Product Citations

Kusumika Saha, .et al. Pharmacological chaperone-rescued cystic fibrosis CFTR-F508del mutant overcomes PRAF2-gated access to endoplasmic reticulum exit sites, Cell Mol Life Sci, 2022, Sep 27;79(10):530 PMID: 36167862
Heledd H Jarosz-Griffiths, .et al. Different CFTR Modulator Combinations Downregulate Inflammation Differently in Cystic Fibrosis, Elife, 2020, Mar 2;9:e54556 PMID: 32118580
Okiyoneda T, .et al. Chaperone-Independent Peripheral Quality Control of CFTR by RFFL E3 Ligase, Dev Cell, 2018, Mar 26;44(6):694-708.e7 PMID: 29503157
Junko Kido, .et al. Cystic Fibrosis Transmembrane Conductance Regulator Reduces Microtubule-Dependent Campylobacter jejuni Invasion, Infect Immun, 2017, Oct; 85(10): e00311-17 PMID: 28784926

Technical details

Catalog Num	A10986
M. Wt	452.4
Formula	C24H18F2N2O5
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	936727-05-8
Synonyms	VX809
SMILES	CC1=C(N=C(C=C1)NC(=O)C2(CC2)C3=CC4=C(C=C3)OC(O4)(F)F)C5=CC(=CC=C5)C(=O)O

Biological Activity

Targets

F508del-CFTR (Fisher rat thyroid cells)
0.1 μM(EC50)

Solubility *

In vitro (25°C)	DMSO	88 mg/mL (194.51 mM)
	Water	Insoluble
	Ethanol	6 mg/mL (13.26 mM)
In vivo	30% PEG400+0.5% Tween80+5% propylene glycol	28 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	22.1 mL	110.52 mL	221.04 mL
0.5 mM	4.42 mL	22.1 mL	44.21 mL
1 mM	2.21 mL	11.05 mL	22.1 mL
5 mM	0.44 mL	2.21 mL	4.42 mL

*The above data is based on the productmolecular weight 452.4 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.