Amenamevir

SKU: orb1303043

Description

Amenamevir

Research Area

Cell Biology, Infectious Disease & Virology, Molecular Biology

Key Properties

• CAS Number: 841301-32-4
• MW: 482.55
• Purity: 99.00%
• Formula: C₂₄H₂₆N₄O₅S
• SMILES: Cc1cccc(C)c1N(CC(=O)Nc1ccc(cc1)-c1ncon1)C(=O)C1CCS(=O)(=O)CC1
• Target: HSV,DNA/RNA Synthesis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.14 mM);DMSO:50 mg/mL (103.62 mM)

Bioactivity

• Target IC50:
  Helicase-primase:14 ng/mL|HSV1:7.7-20 ng/mL|HSV2:15-58 ng/mL
• In Vivo:
  Amenamevir (ASP2151, 3-30 mg/kg/day) dose-dependently accelerates the reduction in virus titer. Amenamevir dose-dependently decreases both HSV-1 titers and lesion scores, irrespective of the dosing interval. Based on the correlation curves, HSV-1 growth is completely inhibited by Amenamevir (p.o.), and these PK parameters are estimated: Cmax in serum, 10,000 ng/mL or higher; AUC24h, 60 μg h/ml or higher; 21 to 24 h for T> 100. The mean concentration of Amenamevir in plasma at 5 days postinfection dose-dependently increases, with doses of 3 mg Amenamevir/g or higher significantly reducing the intradermal HSV-1 titer.
• In Vitro:
  The mean EC50s of Amenamevir against HSV-1 and HSV-2 are 14 (range, 7.7-20) and 30 ng/mL (range, 15-58), respectively, while those of acyclovir (ACV) is 29 (range, 18-38) and 71 ng/mL (range, 45-95), respectively.
• Cell Research:
  The antiviral activities of Amenamevir 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.
• Animal Research:
  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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, Herpes simplex virus, helicase-primase, HSV, DNASynthesis, DNA Synthesis, Amenamevir, ASP 2151, ASP2151, ASP-2151, RNA Synthesis, RNASynthesis

Compound Identifiers

PubChem CID

11397521