| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 100mg |
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Purity: ≥98%
Amenamevir (formerly ASP2151; ASP-2151) is a HSV (herpes simplex virus) helicase-primase inhibitor with potent antiviral activity against HSVs with EC50 of 14 ng/mL. It an antiviral drug used for the treatment of shingles, acting as an inhibitor of the zoster virus's helicase–primase complex. Amenamevir was approved in Japan for the treatment of shingles in 2017. Amenamevir a novel class of antiviral agent other than nucleoside compounds, such as aciclovir, valaciclovir and famciclovir. Amenamevir 400 and 200 mg were well tolerated as well as valaciclovir. The proportions of patients who experienced drug-related adverse events were 10.0% (25/249), 10.7% (27/252) and 12.0% (30/249) with amenamevir 400 and 200 mg and valaciclovir, respectively. In conclusion, amenamevir 400 mg appears to be effective and well tolerated for treatment of herpes zoster in immunocompetent Japanese patients.
| Targets |
HSV-1(IC50=7.7-20 ng/mL);HSV-2(IC50=15-58 ng/mL)
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|---|---|
| ln Vitro |
Amenamevir (ASP2151) prevents the replication of both laboratory-stocked HSV strains and strains isolated in the US and Japan. Acyclovir (ACV) has mean EC50s against HSV-1 and HSV-2 of 29 (range, 18 to 38) and 71 ng/mL (range, 45 to 95), respectively, while amenamevir's mean EC50s against HSV-1 and HSV-2 are 14 (range, 7.7 to 20) and 30 ng/mL (range, 15 to 58), respectively. Compared to ACV, Amenamevir's EC50s against HSV strains are noticeably lower[1].
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| ln Vivo |
The administration of amenamevir (ASP2151) in the dose-dependent range of 3 to 30 mg/kg/day accelerates the reduction in virus titer. Regardless of the dosing interval, amenamevir treatment reduces lesion scores and HSV-1 titers in a dose-dependent manner. The PK parameters at which oral administration of Amenamevir completely suppresses HSV-1 growth are estimated based on the correlation curves. These parameters are 10,000 ng/mL or higher for the maximum concentration of drug in serum (Cmax), 60 μg • h/ml or higher for concentration-time curve over 24 h (AUC24h), and 21 to 24 h for T>100. Five days after infection, the mean plasma concentration of Amenamevir rises in a dose-dependent manner; doses of 3 mg Amenamevir/g or more markedly lower the intradermal HSV-1 titer[1].
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| Cell Assay |
Plaque reduction assay is used to evaluate the antiviral efficacy of Amenamevir (ASP2151) and ACV against HSVs. In a nutshell, HEF cells are cultivated in multiwell plates and allowed to grow into a monolayer. Following the removal of the medium, HSV-1 or HSV-2 is added to the cells, and the plates are then incubated for an additional hour at 37°C. After twice washing the cells in maintenance medium, the test compound—which includes amenamevir—is applied to the cells until clear plaques start to form.After staining the cells with 0.02% crystal violet solution and fixing them with 10% formalin in phosphate-buffered saline, the number of plaques is counted under a light microscope. Using a sigmoid-maximum effect (Emax) model in nonlinear regression analysis, the EC50, or the concentration of test compound required to reduce the plaque number by 50%, is determined[1].
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| Animal Protocol |
Female hairless mice (HOS:HR-1, 7 to 8 weeks old) are infected in the dorsolateral skin stripped as a small square using a needle under anesthesia with a suspension of HSV-1 strains WT51 (15 μL/mouse; titer, 2×108 PFU/mL) or CI-116 (15 μL/mouse; titer, 4×107 PFU/mL). Day zero postinfection is the day of HSV-1 infection. HSV-1-infected mice (n=5) are given oral doses of 1, 3, 10, 30, or 100 mg/kg/day of ASP2151 for a duration of 5 days. Treatments with amenamevir (ASP2151) begin two to three hours after HSV infection. The medication is taken once daily (every 24 hours, q24h), twice a day (every 12 hours, q12h), or three times a day (every 8 hours, q8h). On day five after infection, lesion scores and intradermal HSV-1 titers are measured[1].
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| References |
| Molecular Formula |
C24H26N4O5S
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|---|---|
| Molecular Weight |
482.55
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| Exact Mass |
482.16
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| Elemental Analysis |
C, 59.74; H, 5.43; N, 11.61; O, 16.58; S, 6.64
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| CAS # |
841301-32-4
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| Related CAS # |
1039623-01-2 (LB-80380 maleate)
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| Appearance |
Solid powder
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| SMILES |
O=C(C(CC1)CCS1(=O)=O)N(C2=C(C)C=CC=C2C)CC(NC3=CC=C(C4=NOC=N4)C=C3)=O
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| InChi Key |
MNHNIVNAFBSLLX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H26N4O5S/c1-16-4-3-5-17(2)22(16)28(24(30)19-10-12-34(31,32)13-11-19)14-21(29)26-20-8-6-18(7-9-20)23-25-15-33-27-23/h3-9,15,19H,10-14H2,1-2H3,(H,26,29)
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| Chemical Name |
N-(2-((4-(1,2,4-oxadiazol-3-yl)phenyl)amino)-2-oxoethyl)-N-(2,6-dimethylphenyl)tetrahydro-2H-thiopyran-4-carboxamide 1,1-dioxide
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| Synonyms |
ASP-2151; ASP2151; ASP 2151
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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 : 50~96 mg/mL ( 103.62~198.94 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.31 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 (4.31 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 (4.31 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 (4.31 mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0723 mL | 10.3616 mL | 20.7232 mL | |
| 5 mM | 0.4145 mL | 2.0723 mL | 4.1446 mL | |
| 10 mM | 0.2072 mL | 1.0362 mL | 2.0723 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.
 Reducing effect of ASP2151 on intradermal HSV-1 titers.Antimicrob Agents Chemother.2013 Mar;57(3):1339-46. |
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 Concentrations of ASP2151 in plasma after single or repeated oral administration to mice.Antimicrob Agents Chemother.2013 Mar;57(3):1339-46. |
 Relationship between intradermal HSV-1 titer and three pharmacokinetic (PK) parameters.Antimicrob Agents Chemother.2013 Mar;57(3):1339-46. |
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