| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
FDL-169 targets the CFTR protein, specifically the F508del mutant form that is misfolded and retained in the endoplasmic reticulum. As a CFTR corrector, it binds to the mutant protein and promotes proper folding and trafficking to the cell surface, where it can function as a chloride channel.
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| ln Vitro |
FDL-169 increases the cell surface abundance of Phe508del CFTR. By correcting the folding defect of the mutant protein, it restores CFTR function and improves chloride transport in airway epithelial cells. The compound is designed to fix and restore the function of the defective CFTR protein.
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| ln Vivo |
In vivo activity data for FDL-169 are limited. As a CFTR corrector, it has potential utility in cystic fibrosis patients with the F508del mutation. The compound would need to be evaluated in animal models of CF or in human clinical trials to demonstrate efficacy in improving lung function and reducing disease complications.
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| Enzyme Assay |
Cell-free assays for FDL-169 are not typically performed as CFTR corrector activity requires the context of the cellular folding and trafficking machinery. Biochemical assays using purified CFTR protein could potentially assess direct binding, but functional correction is best measured in cell-based systems.
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| Cell Assay |
Cells expressing F508del CFTR (e.g., CFBE41o- bronchial epithelial cells or primary human bronchial epithelial cells from CF patients) are treated with FDL-169 at various concentrations. CFTR cell surface expression is assessed by cell surface biotinylation followed by Western blot, or by immunofluorescence. CFTR function (chloride transport) is measured using Ussing chamber or fluorescence-based halide-sensitive dye assays.
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| Animal Protocol |
In vivo animal studies for FDL-169 have not been extensively reported. For CFTR corrector development, studies are typically conducted in mouse models expressing human F508del CFTR or in ferret models. The compound could be administered via oral or inhalation routes. Efficacy endpoints would include CFTR function in airway tissues, lung histology, and survival.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of FDL-169 have been characterized in preclinical studies. As a small molecule (MW 486.49, formula C27H23FN4O4), it is expected to have reasonable oral bioavailability. The compound is likely metabolized via hepatic pathways. Detailed PK parameters would be available from development studies.
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| Toxicity/Toxicokinetics |
Toxicity data for FDL-169 are limited. As a CFTR corrector, standard toxicological assessments would be required for clinical development. The compound's selectivity for the F508del mutant over wild-type CFTR and other proteins would determine its safety profile. Gastrointestinal and hepatic effects are common with small molecule CFTR modulators.
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| References | |
| Additional Infomation |
FDL-169 (molecular formula C27H23FN4O4, MW 486.49) is a novel and potent CFTR corrector developed for cystic fibrosis patients with the F508del mutation. It was developed by Flatley Discovery Lab. The compound is designed to fix and restore the function of the defective CFTR protein. It is intended for research use only.
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| Molecular Formula |
C27H23FN4O4
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|---|---|
| Molecular Weight |
486.494329690933
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| Exact Mass |
486.17
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| CAS # |
1628416-28-3
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| PubChem CID |
86298861
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| Appearance |
White to off-white solid powder
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| LogP |
4.6
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
36
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| Complexity |
856
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1=CC=CC(=C1)C1C2C=CC(=CC=2C(N(CC(N(C)C2=CC=C3C(=C2)OC(C)=N3)=O)N=1)=O)OCC
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| InChi Key |
XRPSUWYWZUQALB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H23FN4O4/c1-4-35-20-9-10-21-22(14-20)27(34)32(30-26(21)17-6-5-7-18(28)12-17)15-25(33)31(3)19-8-11-23-24(13-19)36-16(2)29-23/h5-14H,4,15H2,1-3H3
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| Chemical Name |
2-(7-ethoxy-4-(3-fluorophenyl)-1-oxophthalazin-2(1h)-yl)-n-methyl-n-(2-methylbenzo[d]oxazol-6-yl)acetamide
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| Synonyms |
FDL-169; FDL169; FDL 169;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~128.47 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0555 mL | 10.2777 mL | 20.5554 mL | |
| 5 mM | 0.4111 mL | 2.0555 mL | 4.1111 mL | |
| 10 mM | 0.2056 mL | 1.0278 mL | 2.0555 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.