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| Targets |
GFP16 targets the prion protein (PrP) or prion propagation pathways, though the precise molecular target has not been fully characterized. As a low-affinity antiprion compound, GFP16 is believed to interact with the prion protein or modulate cellular pathways involved in prion replication and toxicity. The compound's low affinity suggests that it may bind to its target with relatively weak interactions, which could be useful for studying the structure-activity relationships of antiprion compounds or for identifying more potent derivatives. Prion diseases are caused by the conformational conversion of the cellular prion protein (PrPC) to the pathogenic scrapie form (PrPSc), and compounds that inhibit this conversion or promote PrPSc clearance are of therapeutic interest. GFP16 serves as a tool for investigating these mechanisms.
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| ln Vitro |
In vitro, GFP16 has been characterized as a low-affinity antiprion compound. The compound is used in cell-based assays to evaluate its ability to inhibit prion propagation or reduce prion toxicity in cultured cells. As a low-affinity compound, GFP16 may exhibit limited potency in vitro, but it can serve as a valuable reference compound for structure-activity relationship studies or as a starting point for the development of more potent antiprion agents. The compound's antiprion activity has been demonstrated in research settings, though specific IC50 values and detailed activity data are not extensively documented in publicly available sources. GFP16 may be utilized in combination with other antiprion compounds to study synergistic effects or mechanisms of action.
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| ln Vivo |
In vivo activity of GFP16 has not been extensively documented in publicly available sources. As a low-affinity antiprion compound, GFP16 is primarily used as a research tool for in vitro studies of prion biology and antiprion drug discovery. The compound's low affinity may limit its efficacy in vivo, as higher-affinity compounds are typically required for significant activity in animal models of prion disease. However, GFP16 could be used to study the pharmacokinetic and pharmacodynamic properties of antiprion compounds or to validate screening assays for identifying more potent antiprion agents. Specific in vivo efficacy data in animal models of prion disease has not been reported in publicly available literature.
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| Enzyme Assay |
The antiprion activity of GFP16 is typically assessed using cell-based assays that measure the inhibition of prion propagation. In these assays, prion-infected cells (such as ScN2a cells, which are stably infected with mouse-adapted prions) are treated with varying concentrations of GFP16. After treatment, cells are lysed and the levels of PrPSc (the pathogenic prion protein isoform) are quantified using immunoassays such as ELISA or Western blotting with antibodies specific for PrPSc. The compound's ability to reduce PrPSc levels is expressed as the concentration required for 50% inhibition (IC50). Cytotoxicity is assessed in parallel using standard cell viability assays to ensure that observed antiprion effects are not due to non-specific toxicity.
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| Cell Assay |
Cellular assays for GFP16 are performed using prion-infected cell lines, most commonly ScN2a cells (mouse neuroblastoma cells stably infected with the RML or 22L strain of mouse-adapted prions). Cells are cultured in appropriate growth medium and treated with varying concentrations of GFP16 for specified time periods (typically several days). After treatment, cells are harvested and lysed, and PrPSc levels are quantified using immunoassays. Proteinase K digestion is often used to differentiate PrPSc from PrPC, as PrPSc is partially resistant to proteinase K digestion while PrPC is completely digested. Cell viability is assessed using MTT, CellTiter-Glo, or similar assays to confirm that the compound does not cause non-specific cytotoxicity at the concentrations tested.
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| Animal Protocol |
In vivo studies for GFP16 have not been extensively documented. For antiprion compounds in general, typical in vivo experimental designs involve administration to mouse models of prion disease, such as mice intracerebrally or intraperitoneally inoculated with mouse-adapted prion strains (e.g., RML or 22L strains). The compound is typically administered via intraperitoneal (i.p.) injection or oral gavage, with formulation in suitable vehicles such as DMSO, PEG-based solutions, or saline suspensions. Endpoints include survival analysis, assessment of clinical signs of prion disease (such as weight loss, motor dysfunction, and behavioral changes), and histopathological evaluation of brain tissue for PrPSc deposition and spongiform change.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of GFP16 (molecular weight 333.43, molecular formula C21H23N3O) have been partially characterized. The compound has a calculated LogP of 4.2, indicating moderate lipophilicity. For in vitro use, GFP16 is soluble in DMSO at concentrations up to 100 mg/mL (299.91 mM). Storage recommendations include powder storage at -20°C for up to 3 years and solution storage at -80°C for 6 months or -20°C for 1 month, with protection from light. For in vivo administration, the compound can be formulated in vehicles such as 10% DMSO + 5% Tween 80 + 85% saline or 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% saline. Comprehensive PK parameters are not extensively documented.
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| Toxicity/Toxicokinetics |
GFP16 is intended for research use only and is not approved for human therapeutic applications. Comprehensive toxicological evaluations, including acute and repeat-dose toxicity studies in animal models, have not been reported in publicly available sources. The compound's low affinity for its target suggests that off-target effects may be limited, but standard safety pharmacology assessments would be required if the compound were to be considered for therapeutic development. Researchers should handle GFP16 with appropriate safety precautions, including the use of personal protective equipment and proper laboratory practices for handling research chemicals.
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| Additional Infomation |
GFP16 is a research-grade compound used as a chemical tool for studying prion biology and antiprion drug discovery. Prion diseases are fatal neurodegenerative disorders caused by the misfolding of the prion protein, and there are currently no effective treatments available. GFP16 serves as a low-affinity antiprion compound that can be used to study the mechanisms of prion propagation and to identify more potent antiprion agents through structure-activity relationship studies. The compound is also known as WAY-608339 and is available with purity specifications for research use. GFP16 may be utilized in combination with other antiprion compounds to study synergistic effects or mechanisms of action in prion disease research.
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| Molecular Formula |
C21H23N3O
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| Molecular Weight |
333.426824808121
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| Exact Mass |
333.18
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| Elemental Analysis |
C, 75.65; H, 6.95; N, 12.60; O, 4.80
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| CAS # |
749212-56-4
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| PubChem CID |
3633456
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| Appearance |
White to off-white solid powder
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| LogP |
4.2
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
468
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCC1=NC2=CC=CC=C2N1CC(=O)N3CCCC4=CC=CC=C43
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| InChi Key |
LPGODZAJMWRHBX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H23N3O/c1-2-8-20-22-17-11-4-6-13-19(17)24(20)15-21(25)23-14-7-10-16-9-3-5-12-18(16)23/h3-6,9,11-13H,2,7-8,10,14-15H2,1H3
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| Chemical Name |
1-(3,4-dihydroquinolin-1(2H)-yl)-2-(2-propyl-1H-benzo[d]imidazol-1-yl)ethan-1-one
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| Synonyms |
GFP16; GFP-16; GFP 16
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.9991 mL | 14.9957 mL | 29.9913 mL | |
| 5 mM | 0.5998 mL | 2.9991 mL | 5.9983 mL | |
| 10 mM | 0.2999 mL | 1.4996 mL | 2.9991 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.
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