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- 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
Biological Activity
VX-809 is the second investigational oral candidate compound for the treatment of cystic fibrosis (CF).
Targets
| F508del-CFTR (Fisher rat thyroid cells) | ||||
| 0.1 μM(EC50) |
| 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. |
|||
| 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.
| Catalog Num | A10986 |
|---|---|
| Actions | Modulator |
| CAS No. | 936727-05-8 |
| Formula | C24H18F2N2O5 |
| M. Wt | 452.4 |
| Purity | >98% |
| 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 |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
Datasheet
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