Presatovir (GS-5806)是一种新型的、口服生物利用度高的呼吸道合胞病毒（RSV）融合抑制剂，具有治疗婴幼儿和成人RSV感染的潜力。
Cas No.:1353625-73-6
Sample solution is provided at 25 µL, 10mM.
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Presatovir (GS-5806) is a novel, orally bioavailable RSV fusion inhibitor with the potential to treat RSV infection in infants and adults[1].
In vitro, Presatovir exhibited strong antiviral activity against virus-infected HEp-2 cells, with a mean EC50 value of 0.35±0.14nM[2]. Presatovir showed low cytotoxicity in uninfected HEp-2 cells, with a 50% inhibitory concentration (CC50) of 48900±5600nM[2]. Presatovir inhibited RSV A2 replication in the HAE cell model with a mean EC50 of 0.37±0.28nM[2]. Presatovir antiviral activities against the RSV A and B subtypes were comparable, with mean EC50 of 0.51±0.25nM and 0.35±0.15nM, respectively[2].
References:
[1] Mackman RL, Sangi M, Sperandio D, et al. Discovery of an oral respiratory syncytial virus (RSV) fusion inhibitor (GS-5806) and clinical proof of concept in a human RSV challenge study. J Med Chem. 2015;58(4):1630-1643.
[2] Perron M, Stray K, Kinkade A, et al. GS-5806 Inhibits a Broad Range of Respiratory Syncytial Virus Clinical Isolates by Blocking the Virus-Cell Fusion Process. Antimicrob Agents Chemother. 2015;60(3):1264-1273.
Presatovir (GS-5806)是一种新型的、口服生物利用度高的呼吸道合胞病毒（RSV）融合抑制剂，具有治疗婴幼儿和成人RSV感染的潜力[1]。
在体外，Presatovir对病毒感染的HEp-2细胞表现出较强的抗病毒活性，平均EC50值为0.35±0.14nM[2]。Presatovir对未感染HEp-2细胞具有较低的细胞毒性，半数细胞毒性浓度（CC50）为48900±5600nM[2]。Presatovir在HAE细胞模型中抑制RSV A2复制，平均EC50为0.37±0.28nM[2]。Presatovir对RSV A和B亚型的抗病毒活性的平均EC50分别为0.51±0.25nM和0.35±0.15nM[2]。
| Cell experiment [1]: | |
Cell lines | HEp-2 cells |
Preparation Method | HEp-2 cells were seeded in 6-well plates at a density of 2×105 cells per well, allowed to attach overnight, and infected with either RSV A2 or RSV B 18537 at a multiplicity of infection (MOI) of 0.05PFU/cell. The antiviral activity of Presatovir was detected by gradually increasing the concentration (0.7-350nM). |
Reaction Conditions | 0.7-350nM; 4d |
Applications | Presatovir exhibited potent antiviral activity, with a mean EC50 of 0.35±0.14nM in HEp-2 cells. |
References: | |
| Cas No. | 1353625-73-6 | SDF | |
| 别名 | GS-5806 | ||
| Canonical SMILES | O=C(C(C=C(Cl)C=C1)=C1NS(C)(=O)=O)N(CCCC2)[C@@H]2C3=NN4C(N=C(N5CC[C@H](N)C5)C(C)=C4)=C3 | ||
| 分子式 | C24H30ClN7O3S | 分子量 | 532.06 |
| 溶解度 | DMSO : 6 mg/mL (11.28 mM);Water : < 0.1 mg/mL (insoluble) | 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8795 mL | 9.3974 mL | 18.7949 mL |
| 5 mM | 375.9 μL | 1.8795 mL | 3.759 mL |
| 10 mM | 187.9 μL | 939.7 μL | 1.8795 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% Appearance: A solid
- COA (Certificate of Analysis)
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- Datasheet