1. Anti-infection
  2. HSV
  3. Amenamevir

Amenamevir (Synonyms: ASP2151)

Cat. No.: HY-14809 Purity: 99.81%
Handling Instructions

Amenamevir is a helicase-primase inhibitor which has potent antiviral activity against HSVs with an EC50 of 14 ng/mL.

For research use only. We do not sell to patients.

Amenamevir Chemical Structure

Amenamevir Chemical Structure

CAS No. : 841301-32-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 752 In-stock
Estimated Time of Arrival: December 31
1 mg USD 228 In-stock
Estimated Time of Arrival: December 31
5 mg USD 708 In-stock
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10 mg USD 1188 In-stock
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50 mg USD 3588 In-stock
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100 mg USD 4788 In-stock
Estimated Time of Arrival: December 31
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Description

Amenamevir is a helicase-primase inhibitor which has potent antiviral activity against HSVs with an EC50 of 14 ng/mL.

IC50 & Target

EC50: 14 ng/mL (HSV)[1]

In Vitro

Amenamevir (ASP2151) inhibits the replication of the HSV strains isolated in Japan and the United States as well as the laboratory-stocked strains. The mean EC50s of Amenamevir against HSV-1 and HSV-2 are 14 (range, 7.7 to 20) and 30 ng/mL (range, 15 to 58), respectively, whereas those of acyclovir (ACV) are 29 (range, 18 to 38) and 71 ng/mL (range, 45 to 95), respectively. The EC50s of Amenamevir against HSV strains are significantly lower than those of ACV[1].

In Vivo

Amenamevir (ASP2151) administration accelerates the reduction in virus titer in a dose-dependent manner in the range of 3 to 30 mg/kg/day. Amenamevir treatment decreases both lesion scores and HSV-1 titers in a dose-dependent manner, irrespective of the dosing interval. Based on the correlation curves, the PK parameters at which HSV-1 growth is completely suppressed by oral administration of Amenamevir are estimated to be 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 . The mean concentration of Amenamevir in plasma at 5 days postinfection increases in a dose-dependent manner, with doses of 3 mg Amenamevir/g or higher significantly reducing the intradermal HSV-1 titer[1].

Molecular Weight

482.55

Formula

C₂₄H₂₆N₄O₅S

CAS No.

841301-32-4

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

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (103.62 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.31 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.31 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.31 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

The antiviral activities of Amenamevir (ASP2151) and ACV against HSVs are tested using a plaque reduction assay. Briefly, HEF cells are seeded into multi well plates and incubated until they form a monolayer. After the medium is removed, the cells are infected with HSV-1 or HSV-2, and the plates are further incubated for 1 h at 37°C. The cells are washed twice with maintenance medium and then treated with the test compound (including Amenamevir) until clear plaques appear. The cells are then fixed with 10% formalin in phosphate-buffered saline, stained with a 0.02% crystal violet solution, and the number of plaques is determined under a light microscope. The EC50, which represents the concentration of test compound needed to reduce the plaque number by 50%, is calculated using nonlinear regression analysis with a sigmoid-maximum effect (Emax) model[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Female hairless mice (HOS:HR-1, 7 to 8 weeks old) are infected with a suspension of HSV-1 strain WT51 (15 μL/mouse; titer, 2×108 PFU/mL) or CI-116 (15 μL/mouse; titer, 4×107 PFU/mL) in the dorsolateral skin stripped as a small square using a needle, under anesthesia. The day of HSV-1 infection is designated day zero postinfection. Total daily doses of 1, 3, 10, 30, or 100 mg/kg/day ASP2151 are orally administered to HSV-1-infected mice (n=5) for 5 days. Amenamevir (ASP2151) treatments are started 2 to 3 h after HSV infection either as a single daily dose (every 24 h, q24h) or as two (every 12 h, q12h) or three (every 8 h, q8h) divided doses. Lesion scores and intradermal HSV-1 titers are measured on day 5 postinfection[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Amenamevir
Cat. No.:
HY-14809
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