Amenamevir

Category	Herpes simplex Virus (HSV)
CAS	841301-32-4
Description	Amenamevir is a DNA helicase-primase inhibitor. It has anti-HSV activity against herpes simplex keratitis. In Mar 2016, Mahuro completed a phase III trial in Herpes simplex virus infections in Japan.

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Product Information

Synonyms	UNII-94X46KW4AE; ASP2151; N-(2,6-dimethylphenyl)-N-[2-[4-(1,2,4-oxadiazol-3-yl)anilino]-2-oxoethyl]-1,1-dioxothiane-4-carboxamide
IUPAC Name	N-(2,6-dimethylphenyl)-N-[2-[4-(1,2,4-oxadiazol-3-yl)anilino]-2-oxoethyl]-1,1-dioxothiane-4-carboxamide
Molecular Weight	482.55
Molecular Formula	C24H26N4O5S
Canonical SMILES	CC1=C(C(=CC=C1)C)N(CC(=O)NC2=CC=C(C=C2)C3=NOC=N3)C(=O)C4CCS(=O)(=O)CC4
InChI	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)
InChIKey	MNHNIVNAFBSLLX-UHFFFAOYSA-N
Purity	98%
Solubility	Soluble in DMSO
Appearance	White to off-white solid
Application	Herpes simplex virus infections; Herpes zoster
Shelf Life	2 month in rt, long time
Storage	-20°C Freezer
Animal Admin	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.
Complexity	800
Exact Mass	482.16200
In Vitro	Amenamevir (ASP2151) inhibits the replication of the HSV 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.
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. 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.
PSA	130.85000
Target	EC50: 14 ng/mL (HSV)
XLogP3-AA	2.6