VX-661 (Synonyms: Tezacaftor) |
Catalog No.GC14920
One-Click Copy Product Info
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VX-661 (VX-661) is a second F508del CFTR corrector and help CFTR protein reach the cell surface.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1152311-62-0
Sample solution is provided at 25 µL, 10mM.
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VX-661, one of vertex derivatives, corrects F508del-CFTR trafficking and increases F508del-CFTR protein activity in vitro [1].
VX-661 treated alone or in combination with ivacaftor have shown to enhance F508del-CFTR trafficking to the cell surface. VX-661 has been at phase 2 study [1].
References:
[1] S. Donaldson, J. Pilewski, M. Griese, Q. Dong, P.-S. Lee, for the VX11–661-101 Study Group. WS7.3 VX-661, an investigational CFTR corrector, in combination with ivacaftor, a CFTR potentiator, in patients with CF and homozygous for the F508Del-CFTR mutation: Interim analysis. Journal of Cystic Fibrosis, Volume 12, Supplement 1, June 2013, Page S14
| Cell experiment [1]: | |
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Cell lines |
human CF bronchial epithelial cell line CFBE41o |
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Preparation method |
The solubility of this compound in DMSO ＞21.8mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
3 μM for 24 hours at 26°C. |
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Applications |
VX-661 could partially revert the folding and processing defects and rescue PM(plasma membrane) densities of ΔF508-CFTR(Cystic fibrosis transmembrane regulator). VX-770 was a potentiators that increase channel gating and conductance.VX-770 reduced the correction efficacy of corrector VX-661. The VX-770 effect was attenuated in VX-661 treated cells, probably due to partial stabilization of the mature ΔF508-CFTR pool. A combination of chronic VX-661 and acute VX-770, together with a cAMP (cyclic adenosine 3′,5′-monophosphate) agonist, increased ΔF508-CFTR conductance to ~25% of that in non-CF HBE (human bronchial epithelial). |
| Clinical experiment [2]: | |
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Disease models |
CF (Cystic fibrosis) patients who were homozygous or heterozygous for the F508del mutation. |
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Dosage form |
10,30, 100, or 150 mg daily in oral for 28 days |
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Application |
Interim results found decreases in sweat chloride with VX-661 alone and in combination with ivacaftor(VX-770). A relative change in FEV1 (forced expiratory volume in one second) compared with placebo was significant at 28 days with VX-661 100 mg (9%) and 150 mg (7.5%) in combination with ivacaftor. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] S. Donaldson, J. Pilewski, M. Griese, Q. Dong, P.-S. Lee, for the VX11–661-101 Study Group. WS7.3 VX-661, an investigational CFTR corrector, in combination with ivacaftor, a CFTR potentiator, in patients with CF and homozygous for the F508Del-CFTR mutation: Interim analysis. Journal of Cystic Fibrosis, Volume 12, Supplement 1, June 2013, Page S14 [2] National Institutes of Health. Study of VX-661 Alone and in Combination With Ivacaftor in Subjects Homozygous or Heterozygous to the F508del-Cystic Fibrosis Transmembrane Conductance Regulator(CFTR) Mutation (February 1, 2012). Available at: http://clinicaltrials.gov/ct2/show/NCT01531673. Accessed May 5, 2015. |
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| Cas No. | 1152311-62-0 | SDF | |
| Synonyms | Tezacaftor | ||
| Chemical Name | 1-(2,2-difluoro-1,3-benzodioxol-5-yl)-N-[1-[(2R)-2,3-dihydroxypropyl]-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)indol-5-yl]cyclopropane-1-carboxamide | ||
| Canonical SMILES | CC(C)(CO)C1=CC2=CC(=C(C=C2N1CC(CO)O)F)NC(=O)C3(CC3)C4=CC5=C(C=C4)OC(O5)(F)F | ||
| Formula | C26H27F3N2O6 | M.Wt | 520.5 |
| Solubility | ≥ 21.8mg/mL in DMSO | Storage | Store at -20°C , stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9212 mL | 9.6061 mL | 19.2123 mL |
| 5 mM | 384.2 μL | 1.9212 mL | 3.8425 mL |
| 10 mM | 192.1 μL | 960.6 μL | 1.9212 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)