ALS-8112

目錄號(hào): HY-12983 純度: 98.90%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南技術(shù)支持

ALS-8112是高效，選擇性的呼吸道合胞病毒（RSV）聚合酶抑制劑。5'-三磷酸形式的ALS-8112抑制RSV聚合酶，IC₅₀值為0.02 μM。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

我們將采用定制合成服務(wù)的方式為您快速提供所需產(chǎn)品和技術(shù)服務(wù)

ALS-8112 Chemical Structure

CAS No. : 1445379-92-9

1. 客戶(hù)無(wú)需承擔(dān)相應(yīng)的運(yùn)輸費(fèi)用。

2. 同一機(jī)構(gòu)（單位）同一產(chǎn)品試用裝僅限申領(lǐng)一次，同一機(jī)構(gòu)（單位）一年內(nèi)

可免費(fèi)申領(lǐng)三個(gè)不同產(chǎn)品的試用裝。

3. 試用裝只面向終端客戶(hù)。

規(guī)格	價(jià)格	是否有貨
10 mM * 1 mL in DMSO	￥4846	In-stock
1 mg	￥1500	In-stock
5 mg	￥3500	In-stock
10 mg	￥5000	In-stock
50 mg		詢(xún)價(jià)
100 mg		詢(xún)價(jià)

or 大包裝詢(xún)價(jià)

* Please select Quantity before adding items.

Customer Review

Other Forms of ALS-8112:

Lumicitabine In-stock

MCE 顧客使用本產(chǎn)品發(fā)表的 2 篇科研文獻(xiàn)

•Microorganisms. 2023 Jun 18, 11(6), 1608.
•Antiviral Res. 2018 Feb;150:79-92. [Abstract]

Proliferation Assay

: ALS-8112 purchased from MCE. Usage Cited in: Antiviral Res. 2018 Feb;150:79-92. [Abstract]; To confirm the antiviral effect of StA-NS2-2, infectious titer produced from compound-treated A549 cells and IFN-deficient Vero cells are examined. The RSV polymerase inhibitor ALS-8112 potently inhibits RSV in both cell types.

ALS-8112 相關(guān)產(chǎn)品

•相關(guān)化合物庫(kù):

Bioactive Compound Library Plus

•同靶點(diǎn)產(chǎn)品:

•同靶點(diǎn)蛋白產(chǎn)品:

生物活性
實(shí)驗(yàn)參考方法
純度 & 產(chǎn)品資料
參考文獻(xiàn)

生物活性

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

IC₅₀ & Target

IC50: 0.02 μM (RSV)^[1]

細(xì)胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
HeLa	CC₅₀	> 100 μM Compound: 2c	Cytotoxicity against human HeLa cells assessed as cell viability by CellTiter-Glo luminescent assay Cytotoxicity against human HeLa cells assessed as cell viability by CellTiter-Glo luminescent assay	[PMID: 25667954]
HeLa	EC₅₀	0.15 μM Compound: 2c	Antiviral activity against Respiratory syncytial virus subgenomic replicon system in 395 HeLa cells assessed as reduction in viral replication after 7 days by renilla luciferase assay Antiviral activity against Respiratory syncytial virus subgenomic replicon system in 395 HeLa cells assessed as reduction in viral replication after 7 days by renilla luciferase assay	[PMID: 25667954]
HEp-2	CC₅₀	> 100 μM Compound: ALS-8112	Cytotoxicity against human Hep2 cells assessed as reduction in cell viability measured after 5 days by MTS assay Cytotoxicity against human Hep2 cells assessed as reduction in cell viability measured after 5 days by MTS assay	[PMID: 32143992]
HEp-2	EC₅₀	0.92 μM Compound: 15	Antiviral activity against RSV A2 infected in human Hep2 cells assessed as protection against virus-induced cytopathic effect after 4 days by Cell-Titer Glo assay Antiviral activity against RSV A2 infected in human Hep2 cells assessed as protection against virus-induced cytopathic effect after 4 days by Cell-Titer Glo assay	[PMID: 25978965]
HEp-2	IC₅₀	1 μM Compound: 15	Inhibition of RSV A2 RNA-dependent RNA polymerase expressed in human Hep2 cells using ATP, GTP, UTP, CTP and 1.5 uCi [alpha-32P] NTP as substrate assessed as reduction of total radiolabled transcript after 90 mins by agarose gel electrophoresis Inhibition of RSV A2 RNA-dependent RNA polymerase expressed in human Hep2 cells using ATP, GTP, UTP, CTP and 1.5 uCi [alpha-32P] NTP as substrate assessed as reduction of total radiolabled transcript after 90 mins by agarose gel electrophoresis	[PMID: 25978965]
HEp-2	EC₅₀	2.6 μM Compound: ALS-8112	Antiviral activity against Respiratory syncytial virus A strain Long infected in Hep2 cells assessed as reduction in virus-induced cytopathic effect after 5 days by microscopic analysis Antiviral activity against Respiratory syncytial virus A strain Long infected in Hep2 cells assessed as reduction in virus-induced cytopathic effect after 5 days by microscopic analysis	[PMID: 32143992]
HEp-2	EC₅₀	2.6 μM Compound: ALS-8112	Antiviral activity against Respiratory syncytial virus B infected in Hep2 cells assessed as reduction in virus-induced cytopathic effect after 5 days by microscopic analysis Antiviral activity against Respiratory syncytial virus B infected in Hep2 cells assessed as reduction in virus-induced cytopathic effect after 5 days by microscopic analysis	[PMID: 32143992]
MT4	CC₅₀	21 μM Compound: 15	Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by Cell-Titer Glo assay Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by Cell-Titer Glo assay	[PMID: 25978965]

體外研究
(In Vitro)

ALS-8112 的 5'-三磷酸形式 (ALS-8112 -TP) 是該藥物的活性形式，可通過(guò) RNA 合成的鏈終止選擇性抑制 RSV 聚合酶^[2]。
ALS-008112 進(jìn)入呼吸道各種類(lèi)型的上皮細(xì)胞，隨后被磷酸化形成細(xì)胞內(nèi)三磷酸核苷，半衰期約為 29 小時(shí)。三磷酸核苷類(lèi)似物通過(guò)鏈終止方式抑制 RSV 復(fù)制^[3]。
ALS-8112 是一種體外 RSV 復(fù)制的泛菌株抑制劑。ALS-8112 -TP 抑制 RSV–RNP 復(fù)合物的 RNA 轉(zhuǎn)錄活性，抑制劑量成比例，IC₅₀ 為 0.020 ± 0.008 μM^[4]。

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

分子量

293.68

Formula

C₁₀H₁₃ClFN₃O₄

CAS 號(hào)

1445379-92-9

性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性數(shù)據(jù)

細(xì)胞實(shí)驗(yàn)：

DMSO 中的溶解度 : ≥ 47 mg/mL (160.04 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液

濃度溶劑體積質(zhì)量	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

查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

摩爾計(jì)算器
稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

方案一

請(qǐng)依序添加每種溶劑： 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (8.51 mM); 澄清溶液
方案二

請(qǐng)依序添加每種溶劑： 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.51 mM); 澄清溶液

動(dòng)物溶解方案計(jì)算器

請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只

由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量

請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：

DMSO +

Tween-80 +

Saline

如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網(wǎng)站選購(gòu)。，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。

計(jì)算結(jié)果

工作液所需濃度 : mg/mL

儲(chǔ)備液配制方法 : mg 藥物溶于 μL DMSO（母液濃度為 mg/mL）。

您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。

動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。

連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。

請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱（超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。

純度 & 產(chǎn)品資料

純度: 98.90%

選擇批次：

Data Sheet (628 KB) SDS (251 KB)

COA (178 KB) LCMS (94 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

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.
參考文獻(xiàn)	[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. [Content Brief] [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. [Content Brief] [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. [Content Brief] [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. [Content Brief]

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.

參考文獻(xiàn)

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

ALS-8112 相關(guān)分類(lèi)

Infection

完整儲(chǔ)備液配制表

可選溶劑	濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.4051 mL	17.0253 mL	34.0507 mL	85.1267 mL
	5 mM	0.6810 mL	3.4051 mL	6.8101 mL	17.0253 mL
	10 mM	0.3405 mL	1.7025 mL	3.4051 mL	8.5127 mL
	15 mM	0.2270 mL	1.1350 mL	2.2700 mL	5.6751 mL
	20 mM	0.1703 mL	0.8513 mL	1.7025 mL	4.2563 mL
	25 mM	0.1362 mL	0.6810 mL	1.3620 mL	3.4051 mL
	30 mM	0.1135 mL	0.5675 mL	1.1350 mL	2.8376 mL
	40 mM	0.0851 mL	0.4256 mL	0.8513 mL	2.1282 mL
	50 mM	0.0681 mL	0.3405 mL	0.6810 mL	1.7025 mL
	60 mM	0.0568 mL	0.2838 mL	0.5675 mL	1.4188 mL
	80 mM	0.0426 mL	0.2128 mL	0.4256 mL	1.0641 mL
	100 mM	0.0341 mL	0.1703 mL	0.3405 mL	0.8513 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ALS-81121445379-92-9ALS8112ALS 8112RSVRespiratory syncytial virusInhibitorinhibitorinhibit

您最近查看的產(chǎn)品:

產(chǎn)品名稱(chēng)：

* 需求量：

* 客戶(hù)姓名：

* Email：

* 電話：

* 公司或機(jī)構(gòu)名稱(chēng)：

留言給我們：

MedChemExpress (MCE) 只為有資質(zhì)的科研機(jī)構(gòu)、醫(yī)藥企業(yè)基于科學(xué)研究或藥證申報(bào)的用途提供醫(yī)藥研發(fā)服務(wù)，不為任何個(gè)人或者非科研性質(zhì)的、非用于藥證申報(bào)使用等其他用途提供服務(wù)。	站點(diǎn)地圖隱私聲明
滬ICP備15051369號(hào)-4 上海工商滬公網(wǎng)安備31011502019417 滬(浦)應(yīng)急管危經(jīng)許[2021]201709(QFYS) 營(yíng)業(yè)執(zhí)照（三證合一）
Copyright ? 2013-2025 MedChemExpress. All Rights Reserved.

MedChemExpress (MCE) 只為有資質(zhì)的科研機(jī)構(gòu)、醫(yī)藥企業(yè)基于科學(xué)研究或藥證申報(bào)的用途提供醫(yī)藥研發(fā)服務(wù)，不為任何個(gè)人或者非科研性質(zhì)的、非用于藥證申報(bào)使用等其他用途提供服務(wù)。

站點(diǎn)地圖隱私聲明

滬ICP備15051369號(hào)-4

上海工商

滬公網(wǎng)安備31011502019417

滬(浦)應(yīng)急管危經(jīng)許[2021]201709(QFYS)

營(yíng)業(yè)執(zhí)照（三證合一）

成人免费xx,国产又黄又湿又刺激不卡网站,成人性视频app菠萝网站,色天天天天

ALS-8112

Customer Review

Other Forms of ALS-8112:

MCE 顧客使用本產(chǎn)品發(fā)表的 2 篇科研文獻(xiàn)