| 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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| Other Sizes |
| Targets |
HCV replication(EC50= 0.3 μM)
MK-0608 targets viral RNA-dependent RNA polymerase (RdRp) as a nucleoside analog. It is a 7-deaza-2'-C-methyladenosine derivative that acts as a chain terminator during viral RNA synthesis. By inhibiting viral RNA replication, it shows potent antiviral activity against HCV and other flaviviruses. It has an EC50 of 0.3 μM in the HCV subgenomic replicon assay. |
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| ln Vitro |
In vitro, MK-0608 inhibits HCV RNA replication in the subgenomic HCV genotype 1b replicon with an EC50 of 0.3 μM (EC90 = 1.3 μM). It is a nucleoside analog that effectively inhibits the replication of multiple mosquito-borne flaviviruses, including dengue virus (DENV) and Zika virus (ZIKV). Its antiviral activity is mediated through inhibition of viral RNA polymerase.
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| ln Vivo |
When MK-0608 is taken orally, it has a strong antiviral effect. MK-0608 shows good to excellent oral bioavailability (50 to 100%) and long plasma half-lives in dogs and rhesus macaques (9 and 14 h, respectively) in preclinical pharmacokinetic experiments with rats, dogs, and rhesus monkeys[1].
MK-0608 has demonstrated potent antiviral efficacy in vivo. It has shown efficacy against HCV-infected chimpanzees. As an orally bioavailable compound, it has potential for the treatment of HCV and other viral infections. Further studies are needed to evaluate its efficacy in humans. |
| Enzyme Assay |
MK-0608's antiviral activity is assessed using in vitro cell-based assays, such as the subgenomic HCV replicon assay. In this assay, cells harboring the HCV replicon are treated with the compound, and viral RNA replication is measured. The EC50 and EC90 values are determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays for MK-0608 involve treating HCV replicon-containing cells with the compound and measuring viral RNA levels. The compound's ability to inhibit viral replication is assessed by quantifying viral RNA using real-time PCR or other methods. Its effects on cell viability are also evaluated to ensure selectivity.
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| Animal Protocol |
Animal Model: The HCV-infected chimpanzees[1]
Dosage: 1 mg/kg Administration: Administered orally; once daily for 37 days Result: Baseline viral loads for chimpanzees X6 and X4 ranged from 1,110 to 12,900 IU/mL and 3×106 to 9×106 IU/mL, respectively. In vivo animal model protocols for MK-0608 involve its administration to HCV-infected chimpanzees to evaluate its antiviral efficacy. The compound is typically administered orally. Viral load, pharmacokinetic parameters, and safety are assessed. Studies in other animal models of flavivirus infection may also be conducted. |
| ADME/Pharmacokinetics |
MK-0608 is an orally bioavailable compound. It has a molecular weight of 280.28 and a molecular formula of C12H16N4O4. Specific pharmacokinetic data is not extensively detailed in the available literature. As a nucleoside analog, its pharmacokinetic properties would be expected to support oral administration.
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| Toxicity/Toxicokinetics |
The toxicological profile of MK-0608 has not been extensively characterized in the available literature. As a research compound, it is intended for research use only and not for human consumption. Standard safety assessments would be required for clinical development.
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| References | |
| Additional Infomation |
MK-0608 (CAS# 443642-29-3) is a research compound used to study the replication of HCV and other flaviviruses. It is a nucleoside analog and orally bioavailable inhibitor of HCV replication. It is not approved for clinical use and is supplied as a research chemical.
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| Molecular Formula |
C12H16N4O4
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|---|---|
| Molecular Weight |
280.284
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| Exact Mass |
280.117
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| CAS # |
443642-29-3
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| PubChem CID |
3011893
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| Appearance |
White to off-white solid powder
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| Density |
1.8±0.1 g/cm3
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| Boiling Point |
620.7±55.0 °C at 760 mmHg
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| Melting Point |
222 °C(Solv: methanol (67-56-1)
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| Flash Point |
329.2±31.5 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.769
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| LogP |
0.22
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
20
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| Complexity |
373
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C[C@]1([C@@H]([C@H](O[C@H]1N2C=CC3=C(N=CN=C32)N)CO)O)O
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| InChi Key |
IRZRJANZDIOOIF-GAJNKVMBSA-N
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| InChi Code |
InChI=1S/C12H16N4O4/c1-12(19)8(18)7(4-17)20-11(12)16-3-2-6-9(13)14-5-15-10(6)16/h2-3,5,7-8,11,17-19H,4H2,1H3,(H2,13,14,15)/t7-,8-,11-,12-/m1/s1
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| Chemical Name |
(2R,3R,4R,5R)-2-(4-amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-5-(hydroxymethyl)-3-methyltetrahydrofuran-3,4-diol
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| Synonyms |
MK-608 MK608 MK 608MK 0608 MK-0608 MK06087-deaza-2'-C-methyladenosine 7-DMA
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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 : ~250 mg/mL (~891.97 mM）
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.42 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 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: ≥ 2.08 mg/mL (7.42 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.42 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.08 mg/mL (7.42 mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5679 mL | 17.8393 mL | 35.6786 mL | |
| 5 mM | 0.7136 mL | 3.5679 mL | 7.1357 mL | |
| 10 mM | 0.3568 mL | 1.7839 mL | 3.5679 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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