GLPG2451 |
| カタログ番号GC36149 |
GLPG2451 は、嚢胞性線維症膜コンダクタンス レギュレーター (CFTR) 増強剤であり、11.1 nM の EC50 で低温レスキュー F508del CFTR を効果的に増強します 。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2055015-61-5
Sample solution is provided at 25 µL, 10mM.
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GLPG2451 is a cystic fibrosis transmembrane conductance regulator (CFTR) potentiator, which effectively potentiates low temperature rescued F508del CFTR with an EC50 of 11.1 nM[1]. Cystic fibrosis transmembrane conductance regulator[1]
GLPG2451 has an EC50 value of 675 nM and an efficacy level of 147% of that of VX770 in G551D/F508del cells[1].
[1]. Gees M, et al. Identification and Characterization of Novel CFTR Potentiators. Front Pharmacol. 2018 Oct 26;9:1221.
| Cas No. | 2055015-61-5 | SDF | |
| Canonical SMILES | O=S(C1=CC=C(OC(F)(F)F)C=C1)(C2=CN=C(C(NC[C@@H](O)C)=O)C(N)=C2)=O | ||
| Formula | C16H16F3N3O5S | M.Wt | 419.38 |
| 溶解度 | DMSO: 270 mg/mL (643.81 mM) | Storage | Store at -20°C |
| 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 | 2.3845 mL | 11.9224 mL | 23.8447 mL |
| 5 mM | 0.4769 mL | 2.3845 mL | 4.7689 mL |
| 10 mM | 0.2384 mL | 1.1922 mL | 2.3845 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 ddH2O, 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)
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