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Amenamevir

Amenamevir

产品编号 T4226   CAS 841301-32-4
别名: ASP2151, 阿莫奈韦

Amenamevir (ASP2151) 是一种新型解旋酶引发酶抑制剂,对水痘带状疱疹病毒和 1 型和 2 型单纯疱疹病毒具有活性,EC50值为 14 ng/mL。

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Amenamevir Chemical Structure
Amenamevir, CAS 841301-32-4
规格 价格/CNY 货期 数量
1 mg ¥ 535 现货
2 mg ¥ 772 现货
5 mg ¥ 1,230 现货
10 mg ¥ 1,980 现货
25 mg ¥ 3,590 现货
50 mg ¥ 5,190 现货
100 mg ¥ 7,330 现货
500 mg ¥ 14,600 现货
1 mL * 10 mM (in DMSO) ¥ 1,280 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
Doxorubicin hydrochloride限时半价
产品目录号及名称: Amenamevir (T4226)
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纯度: 99.86%
纯度: 99.00%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Amenamevir (ASP2151) is a novel helicase-primase inhibitor that is active against varicella-zoster virus and herpes simplex virus types 1 and 2 (EC50: 14 ng/mL).
靶点活性 Helicase-primase:14 ng/mL
体外活性 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.
体内活性 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.
细胞实验 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[1].
动物实验 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].
别名 ASP2151, 阿莫奈韦
分子量 482.55
分子式 C24H26N4O5S
CAS No. 841301-32-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 160 mg/mL

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TargetMol Library Books参考文献

1. Katsumata K, et al. Pharmacokinetics and pharmacodynamics of ASP2151, a helicase-primase inhibitor, in a murine model of herpes simplex virus infection. Antimicrob Agents Chemother. 2013 Mar;57(3):1339-46.
Shizukaol B Gemcitabine hydrochloride 2-Keto-D-galactose WRN inhibitor 2 RdRP-IN-6 BMVC-8C3O RAD51 Inhibitor B02 ZYN57939

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 药物功能重定位化合物库 抗癌上市药物库 抗癌临床化合物库 抑制剂库 临床期小分子药物库 抗衰老化合物库 毒性化合物库 DNA 损伤和修复分子库 抗COVID-19化合物库

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体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

Amenamevir 841301-32-4 Cell Cycle/Checkpoint DNA Damage/DNA Repair Microbiology/Virology DNA/RNA Synthesis HSV ASP2151 Herpes simplex virus Inhibitor ASP-2151 ASP 2151 inhibit 阿莫奈韦 inhibitor

 

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