BAY 57-1293
(Synonyms: 普瑞利韦; AIC316; BAY 57-1293) 目录号 : GC11359
A helicase-primase inhibitor
Cas No.:348086-71-5
Sample solution is provided at 25 µL, 10mM.
BAY 57-1293 is a potent and safe inhibitor of HSV helicase-primase with IC50 value of 12nM [1].
BAY 57-1293 displays anti-herpes activity through inhibiting the helicase-primase and affecting the viral DNA synthesis. In the in vitro viral replication assay, BAY 57-1293 shows inhibition against HSV-1 F, HSV-2 G and acyclovir-resistant HSV-1 F mutant with IC50 value of 20nM. In the plaque reduction assay and the conventional cytopathogenicity assay, BAY 57-1293 shows IC50 values of 0.01-0.02μM and 0.01-0.03μM, respectively. Besides that, BAY 57-1293 is active at an IC50 value of 10nM–30nM against all clinical isolates of HSV-1 and HSV-2. Furthermore, BAY 57-1293 is active in vivo. The oral administration of BAY 57-1293 shows 10-fold more potent than valacyclovir in a murine model of disseminated herpes infection. In a rat lethal challenge model, BAY 57-1293 exerts profound antiviral activity without toxic effects. [1, 2]
References:
[1] Kleymann G, Fischer R, Betz U A K, et al. New helicase-primase inhibitors as drug candidates for the treatment of herpes simplex disease. Nature medicine, 2002, 8(4): 392-398.
[2] Betz U A K, Fischer R, Kleymann G, et al. Potent in vivo antiviral activity of the herpes simplex virus primase-helicase inhibitor BAY 57-1293. Antimicrobial agents and chemotherapy, 2002, 46(6): 1766-1772.
Cas No. | 348086-71-5 | SDF | |
别名 | 普瑞利韦; AIC316; BAY 57-1293 | ||
化学名 | N-methyl-N-(4-methyl-5-sulfamoyl-1,3-thiazol-2-yl)-2-(4-pyridin-2-ylphenyl)acetamide | ||
Canonical SMILES | CC1=C(SC(=N1)N(C)C(=O)CC2=CC=C(C=C2)C3=CC=CC=N3)S(=O)(=O)N | ||
分子式 | C18H18N4O3S2 | 分子量 | 402.49 |
溶解度 | ≥ 13.9mg/mL in DMSO | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
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1 mg | 5 mg | 10 mg |
1 mM | 2.4845 mL | 12.4227 mL | 24.8453 mL |
5 mM | 0.4969 mL | 2.4845 mL | 4.9691 mL |
10 mM | 0.2485 mL | 1.2423 mL | 2.4845 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
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