| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
EC90: 0.3 μM (Huh7-Luc cell)[1]. EC50: 82 nM (HCV)[2]
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|---|---|
| ln Vitro |
In Huh7-Luc cells, TMC647055 (choline salt) exhibits antiviral activity with an EC90 value of 0.3 μM[1]. In cellular HCV tests, TMC647055 Choline salt exhibits strong combine action with an EC50 value of 82 nM[2].
|
| ln Vivo |
TMC647055 Compound 18a, choline salt, exhibits a satisfactory pharmacokinetic profile with a single oral dosage of 10 mg/kg, demonstrating good oral bioavailability and systemic exposure, moderate plasma clearance, and a modest volume of distribution[2].
|
| Animal Protocol |
Animal/Disease Models: Rats[2]
Doses: 2 mg/kg; 10mg/kg Route of Administration: 2 mg/kg, iv.; 10mg/kg, po.; singel Experimental Results: No . Cl (L/h/kg) Cmax (ng/mL) [Liver] (ng/mL) L/PF (%) TMC647055 (compound 18a) 3.2 440 7800 46 ＞66 |
| References |
[1]. Devogelaere B, et al. TMC647055, a potent nonnucleoside hepatitis C virus NS5B polymerase inhibitor with cross-genotypic coverage. Antimicrob Agents Chemother. 2012 Sep;56(9):4676-4684.
[2]. Sandrine Vendeville, et al. Finger loop inhibitors of the HCV NS5b polymerase. Part II. Optimization of tetracyclic indole-based macrocycle leading to the discovery of TMC647055. Bioorg Med Chem Lett. 2012 Jul 1;22(13):4437-43. |
| Molecular Formula |
C37H53N5O8S
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|---|---|
| Molecular Weight |
727.91
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| Related CAS # |
TMC647055;1204416-97-6
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 (~85.86 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.86 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3738 mL | 6.8690 mL | 13.7380 mL | |
| 5 mM | 0.2748 mL | 1.3738 mL | 2.7476 mL | |
| 10 mM | 0.1374 mL | 0.6869 mL | 1.3738 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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