Presatovir|1353625-73-6|(GS-5806)-陌孚医药/Medlife

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Presatovir (Synonyms: GS-5806)

目录号: PL11096 纯度: ≥99%

CAS No. :1353625-73-6

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中文名称	Presatovir
英文名称	Presatovir
英文别名	Presatovir;GS-5806;N-[2-[[(2S)-2-[5-[(3S)-3-Amino-1-pyrrolidinyl]-6-methylpyrazolo[1,5-a]pyrimidin-2-yl]-1-piperidinyl]carbonyl]-4-chlorophenyl]methanesulfonamide;GS 5806;BCP17831;N-[2-[(2S)-2-[5-(3-Aminopyrrolidin-1-yl)-6-methylpyrazolo[1,5-a]pyrimidin-2-yl]piperidine-1-carbonyl;9628AJ27JA;Presatovir [USAN:INN];GS5806;Presatovir (USAN/INN);DB12165;Methanesulfonamide, N-(2-(((2S)-2-(5-((3S)-3-amino-1-pyrrolidinyl)-6-methylpyrazolo(1,5-a)pyrimidin-2-yl)-1-piperidinyl)carbonyl)-4-chlorophenyl)-;D11216;Q27271846;N-(2-((S)-2-(5-((S)-3-aminopyrrolidin-1-yl)-6-methylpyrazolo[1,5-a]pyrimidin-2-yl)piperidine-1-carbonyl)-4-chloroph
Cas No.	1353625-73-6
分子式	C₂₄H₃₀ClN₇O₃S
分子量	532.06
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Presatovir (GS-5806) 是一种有效的，具有口服活性的 RSV 融合抑制剂，平均 EC₅₀ 值为 0.43 nM。

生物活性

Presatovir (GS-5806) is an orally bioavailable RSV fusion inhibitor with a mean EC 50 value of 0.43 nM.

性状

Solid

IC50 & Target[1][2]

EC50: 0.43 nM (RSV)

体外研究(In Vitro)

Presatovir is a novel, orally bioavailable RSV fusion inhibitor discovered following a lead optimization campaign on a hit originated from a phenotypic RSV antiviral high-throughput screen. Presatovir exhibits potent activity against a wide range of RSV A and B clinical isolates with a mean EC50 value of 0.43 nM. GS-5806 inhibits pre to post triggered conformational changes of RSV F protein, suggesting a possible mechanism for antiviral activity. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Presatovir demonstrates dose-dependent (0-30 mg/kg) antiviral efficacy in a cotton rat model of RSV infection. Oral bioavailability in preclinical species ranges from 46 to 100%, with penetration of the compound into the lung tissue demonstrated in Sprague-Dawley rats. Multidose oral treatment of Presatovir appears safe in adults, and in healthy human volunteers experimentally infected with RSV, a potent antiviral effect and reduction in disease severity is observed in the high dose group. A group treated with a lower dose of Presatovir allows for a PK-PD relationship to be established to help guide future dose selections. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Mackman RL, 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 Feb 26;58(4):1630-1643.
[2]. Samuel D, et al. GS-5806 inhibits pre- to postfusion conformational changes of the respiratory syncytial virus fusion protein. Antimicrob Agents Chemother. 2015 Nov;59(11):7109-12.

溶解度数据	In Vitro: DMSO : 6 mg/mL (11.28 mM; Need ultrasonic and warming)H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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