Presatovir 纯度:99.95% 5mg

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Presatovir 纯度:99.95% 5mg

市场价：: 3500.00

促销价：: ¥3500.00

货号：HY-16727

品牌：MCE

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商品介绍
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Presatovir (GS-5806) 是新颖且有口服活性的 RSV 融合抑制剂，平均EC₅₀ 值为0.43 nM.

Description

Presatovir (GS-5806) is a novel, orally bioavailable RSV fusion inhibitor with a mean EC₅₀ value of 0.43 nM.

IC₅₀ & Target

EC50: 0.43 nM (RSV)^[1]

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^[1]. GS-5806 inhibits pre to post triggered conformational changes of RSV F protein, suggesting a possible mechanism for antiviral activity^[2].

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^[1].

Solvent & Solubility

In Vitro:

DMSO : 6 mg/mL (11.28 mM; Need ultrasonic and warming)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8795 mL	9.3974 mL	18.7949 mL
5 mM	0.3759 mL	1.8795 mL	3.7590 mL
10 mM	0.1879 mL	0.9397 mL	1.8795 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO 90% corn oil

Solubility: ≥ 0.6 mg/mL (1.13 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 0.6 mg/mL (1.13 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 0.6 mg/mL (1.13 mM); Clear solution

References

[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.

Cell Assay ^[1]	GS-5806 are diluted in 100% DMSO. To conduct the cytopathic antiviral assay, 0.4 μL of 100×concentrated 3-fold serially diluted drug is added to 20 μL of cell culture medium in a 384-well plate. HEp-2 cells are then suspended in MEM plus 10% FBS at a density of 1×10⁵ cells/mL, are infected in bulk with RSV A2 at a titer of approximately 1×10^4.5 tissue culture infectious doses/mL. Immediately following infection, 20 μL of RSV-infected cells are added to each well. The cells are then cultured for 4 days at 37 °C. Following this incubation the cells are allowed to equilibrate to 25°C. The RSV-induced cytopathic effect is determined by adding 40 μL of Cell-Titer Glo viability reagent. Following a 10 min incubation at 25 °C, cell viability is determined^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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.

Cell Assay
^[1]

GS-5806 are diluted in 100% DMSO. To conduct the cytopathic antiviral assay, 0.4 μL of 100×concentrated 3-fold serially diluted drug is added to 20 μL of cell culture medium in a 384-well plate. HEp-2 cells are then suspended in MEM plus 10% FBS at a density of 1×10⁵ cells/mL, are infected in bulk with RSV A2 at a titer of approximately 1×10^4.5 tissue culture infectious doses/mL. Immediately following infection, 20 μL of RSV-infected cells are added to each well. The cells are then cultured for 4 days at 37 °C. Following this incubation the cells are allowed to equilibrate to 25°C. The RSV-induced cytopathic effect is determined by adding 40 μL of Cell-Titer Glo viability reagent. Following a 10 min incubation at 25 °C, cell viability is determined^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References