ALS-8112 纯度:99.15% 100mg

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首页酶、辅酶及抑制剂MCE>

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ALS-8112 纯度:99.15% 100mg

市场价：: 21000.00

促销价：: ¥21000.00

货号：HY-12983

品牌：MCE

配送至：

北京朝阳

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商品介绍
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ALS-8112是高效选择性的呼吸道合胞病毒（RSV）聚合酶的抑制剂。5'-三磷酸ALS-8112抑制RSV聚合酶的IC₅₀值为0.02 μM。

Description

ALS-8112 is a potent and selective respiratory syncytial virus (RSV) polymerase inhibitor. The 5'-triphosphate of ALS-8112 inhibits RSV polymerase with an IC₅₀ of 0.02 μM.

IC₅₀ & Target

IC50: 0.02 μM (RSV)^[1]

In Vitro

The 5'-triphosphate form of ALS-8112 (ALS-8112-TP) is the active form of the drug and selectively inhibits RSV polymerase through chain termination of RNA synthesis^[2]. ALS-008112 enters various types of epithelial cells in the respiratory tract and is subsequently phosphorylated to form an intracellular nucleoside triphosphate with a half-life of approximately 29 hours. The nucleoside triphosphate analogue inhibits RSV replication by means of chain termination^[3]. ALS-8112 is a pan-strain inhibitor of RSV replication in vitro. The RNA transcription activity of the RSV–RNP complex is dose-proportionally inhibited by ALS-8112-TP with an IC₅₀ of 0.020 ± 0.008 μM^[4].

Solvent & Solubility

In Vitro:

DMSO : ≥ 47 mg/mL (160.04 mM)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.4051 mL	17.0253 mL	34.0507 mL
5 mM	0.6810 mL	3.4051 mL	6.8101 mL
10 mM	0.3405 mL	1.7025 mL	3.4051 mL

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

References

[1]. Wang G, et al. Discovery of 4'-chloromethyl-2'-deoxy-3',5'-di-O-isobutyryl-2'-fluorocytidine (ALS-8176), a first-in-class RSV polymerase inhibitor for treatment of human respiratory syncytial virus infection. J Med Chem. 2015 Feb 26;58(4):1862-78.

[2]. Jordan PC, et al. Activation Pathway of a Nucleoside Analog Inhibiting Respiratory Syncytial Virus Polymerase. ACS Chem Biol. 2017 Jan 20;12(1):83-91.

[3]. DeVincenzo JP, et al. Activity of Oral ALS-008176 in a Respiratory Syncytial Virus Challenge Study. N Engl J Med. 2015 Nov 19;373(21):2048-58.

[4]. Deval J, et al. Molecular Basis for the Selective Inhibition of Respiratory Syncytial Virus RNA Polymerase by 2'-Fluoro-4'-Chloromethyl-Cytidine Triphosphate. PLoS Pathog. 2015 Jun 22;11(6):e1004995.

Cell Assay ^[4]	ALS-8112 and its prodrug ALS-8176 are stored at 4°C in dimethyl sulfoxide (DMSO), and diluted in water. HEp-2 cells per well are plated in a 96-well plate. Each compound is serially diluted (1:3) up to 9 distinct concentrations. Cells are pre-incubated with compounds for 24 hours at 37°C in a 5% CO₂ atmosphere. After 24 hours of pre-incubation with compounds, RSV A2, Long, or B1 at a multiplicity of infection (MOI) of 0.5 is added to the cells, except for the background controls. The plate is then incubated for additional 4 days in the same conditions and at the end of the incubation 50 μL the supernatant from each well of the plate is collected^[4]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Wang G, et al. Discovery of 4'-chloromethyl-2'-deoxy-3',5'-di-O-isobutyryl-2'-fluorocytidine (ALS-8176), a first-in-class RSV polymerase inhibitor for treatment of human respiratory syncytial virus infection. J Med Chem. 2015 Feb 26;58(4):1862-78. [2]. Jordan PC, et al. Activation Pathway of a Nucleoside Analog Inhibiting Respiratory Syncytial Virus Polymerase. ACS Chem Biol. 2017 Jan 20;12(1):83-91. [3]. DeVincenzo JP, et al. Activity of Oral ALS-008176 in a Respiratory Syncytial Virus Challenge Study. N Engl J Med. 2015 Nov 19;373(21):2048-58. [4]. Deval J, et al. Molecular Basis for the Selective Inhibition of Respiratory Syncytial Virus RNA Polymerase by 2'-Fluoro-4'-Chloromethyl-Cytidine Triphosphate. PLoS Pathog. 2015 Jun 22;11(6):e1004995.

Cell Assay
^[4]

ALS-8112 and its prodrug ALS-8176 are stored at 4°C in dimethyl sulfoxide (DMSO), and diluted in water. HEp-2 cells per well are plated in a 96-well plate. Each compound is serially diluted (1:3) up to 9 distinct concentrations. Cells are pre-incubated with compounds for 24 hours at 37°C in a 5% CO₂ atmosphere. After 24 hours of pre-incubation with compounds, RSV A2, Long, or B1 at a multiplicity of infection (MOI) of 0.5 is added to the cells, except for the background controls. The plate is then incubated for additional 4 days in the same conditions and at the end of the incubation 50 μL the supernatant from each well of the plate is collected^[4].

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

References