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| Targets |
TTP-8307 targets oxysterol-binding protein (OSBP), a host factor that is essential for the replication of certain viruses. By binding to OSBP, the compound disrupts the intracellular lipid transport and signaling pathways that are hijacked by viruses for their replication. This interaction is crucial for its antiviral activity against a broad range of RNA viruses, including enteroviruses and hepatitis C virus. The compound's selectivity for OSBP over other cellular proteins contributes to its specific antiviral effects without significant cytotoxicity to host cells.
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| ln Vitro |
TTP-8307 inhibits coxsackievirus B3 (CVB3 Nancy) replication with an EC50 of 1.2 μM, targeting non-structural protein 3A. Coxsackievirus B3, three poliovirus Sabin strains, and coxsackieviruses A16 and A21 (EC50 of 0.85 and 5.34 μM) are all inhibited by TTP-8307. Human rhinoviruses (HRV) 2, 29, 39, 45, 63, and 85 are inhibited by TTP-8307. Entovirus replication inhibitor TTP-8307 is resistant to mutations in nonstructural protein 3A [1]. The OSBP-dependent viruses HCV and encephalomyocarditis virus (EMCV) are inhibited by TTP-8307[2].
TTP-8307 demonstrates potent in vitro antiviral activity against multiple viruses. It inhibits coxsackievirus B3 (CVB3) with an EC50 of 1.2 μM and poliovirus by interfering with viral RNA synthesis. The compound also shows activity against coxsackieviruses A16 and A21 with EC50 values of 0.85 and 5.34 μM, respectively. Additionally, TTP-8307 inhibits the replication of the three poliovirus Sabin strains and OSBP-dependent viruses such as EMCV and HCV. These results indicate that TTP-8307 is a broad-spectrum antiviral agent with potent activity against various enteroviruses and other OSBP-dependent viruses. |
| ln Vivo |
In vivo activity data for TTP-8307 are limited in the available literature. However, based on its potent in vitro antiviral activity and its mechanism of action targeting OSBP, the compound is expected to exhibit antiviral efficacy in animal models of enteroviral infection. Further studies are required to evaluate its pharmacokinetic properties, bioavailability, and therapeutic efficacy in vivo. The compound's ability to inhibit viral RNA synthesis and disrupt OSBP-dependent pathways suggests potential for in vivo applications, but comprehensive animal studies have not been extensively reported.
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| Enzyme Assay |
The in vitro enzyme/receptor binding assay for TTP-8307 typically involves evaluating its inhibitory activity against OSBP or viral RNA polymerase in cell-free systems. The assay is performed by incubating the compound with recombinant OSBP or viral replication complexes in the presence of radiolabeled or fluorescent substrates. Binding affinity is determined by measuring the displacement of a known ligand or the inhibition of enzymatic activity. Dose-response curves are generated to calculate IC50 or EC50 values. The assay conditions are optimized to ensure that the compound's solubility and stability are maintained, and appropriate controls are included to validate the specificity of the interaction.
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| Cell Assay |
The in vitro cellular assay for TTP-8307 is conducted using virus-infected mammalian cell lines, such as HeLa or Vero cells. Cells are seeded in multi-well plates and allowed to adhere overnight. The compound is serially diluted in culture medium and added to the cells, followed by infection with the virus at a predetermined multiplicity of infection (MOI). After incubation for a defined period (typically 24-72 hours), viral replication is quantified by measuring the cytopathic effect (CPE), viral RNA levels via qRT-PCR, or plaque reduction assays. The EC50 values are calculated from dose-response curves. Cytotoxicity is assessed in parallel using MTT or similar assays to ensure the observed antiviral effects are not due to cell death.
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| Animal Protocol |
In vivo animal experiments for TTP-8307 would typically involve murine models of enteroviral infection, such as coxsackievirus B3-induced myocarditis or poliovirus infection. The compound would be administered via oral gavage, intraperitoneal injection, or intravenous injection at various doses. Infected animals are monitored for survival, clinical signs, viral load in target organs (e.g., heart, pancreas, or central nervous system), and histopathological changes. Efficacy is evaluated by comparing the treated group with vehicle control and untreated infected groups. Pharmacokinetic parameters may also be assessed to correlate drug exposure with antiviral efficacy. Detailed in vivo protocols for TTP-8307 have not been extensively published.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of TTP-8307 have not been extensively characterized in the available literature. Based on its chemical properties (molecular weight 436.48, LogP not reported), the compound is expected to have moderate oral bioavailability and reasonable tissue distribution. Solubility in DMSO (100 mg/mL) suggests good lipophilicity. Further studies are needed to determine its plasma half-life, clearance, volume of distribution, and protein binding. The compound's PK profile would be essential for optimizing dosing regimens in in vivo efficacy studies and for assessing its potential for further development as an antiviral therapeutic.
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| Toxicity/Toxicokinetics |
Toxicological data for TTP-8307 are limited in the available literature. In vitro cytotoxicity assays typically show that the compound has a favorable selectivity index, as it inhibits viral replication at concentrations well below those that cause significant cytotoxicity to host cells. For example, the EC50 for CVB3 is 1.2 μM, suggesting a reasonable therapeutic window. Comprehensive in vivo toxicology studies, including acute and chronic toxicity, genotoxicity, and organ-specific toxicity, have not been reported. Further safety assessments would be required to evaluate the compound's potential for clinical development.
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| References |
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| Additional Infomation |
TTP-8307 is a research compound that has not yet entered clinical trials or received regulatory approval for therapeutic use. It is primarily used as a tool compound to study the role of OSBP in viral replication and to explore the antiviral potential of OSBP inhibitors. The compound's broad-spectrum activity against enteroviruses and other OSBP-dependent viruses makes it a valuable candidate for further pharmacological development. Additional research is needed to optimize its pharmacokinetic properties, evaluate its efficacy in animal models, and assess its safety profile before it can be considered for clinical applications.
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| Molecular Formula |
C27H21FN4O
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| Molecular Weight |
436.480249166489
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| Exact Mass |
436.169
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| CAS # |
950225-08-8
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| PubChem CID |
16739062
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| Appearance |
White to light yellow solid powder
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| LogP |
4.9
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
33
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| Complexity |
654
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C(C1C=CC=C(C2=CN=C(C3N=CC4C=CC=CC=4C=3)N2)C=1)(=O)N[C@@H](C1C=CC(F)=CC=1)C
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| InChi Key |
SIBDJDZVNXVLEX-QGZVFWFLSA-N
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| InChi Code |
InChI=1S/C27H21FN4O/c1-17(18-9-11-23(28)12-10-18)31-27(33)21-8-4-7-20(13-21)25-16-30-26(32-25)24-14-19-5-2-3-6-22(19)15-29-24/h2-17H,1H3,(H,30,32)(H,31,33)/t17-/m1/s1
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| Chemical Name |
N-[(1R)-1-(4-fluorophenyl)ethyl]-3-(2-isoquinolin-3-yl-1H-imidazol-5-yl)benzamide
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| Synonyms |
TTP-8307TTP 8307TTP8307
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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 : ~100 mg/mL (~229.11 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.73 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (5.73 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2911 mL | 11.4553 mL | 22.9106 mL | |
| 5 mM | 0.4582 mL | 2.2911 mL | 4.5821 mL | |
| 10 mM | 0.2291 mL | 1.1455 mL | 2.2911 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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