Delavirdine mesylate (Synonyms: 地拉夫定甲磺酸盐; U 90152 mesylate; BHAP-U 90152 mesylate)

目录号: HY-10571A 纯度: 99.82%: FAQs
Data Sheet SDS COA 产品使用指南技术支持

Delavirdine (U 90152) mesylate 是一种有效的口服活性非核苷逆转录酶抑制剂 (NNRTI)。Delavirdine mesylate 选择性地抑制 HIV-1 逆转录酶 (HIV-1 RT) (IC₅₀=0.26?μM)，选择性超过 DNA 聚合酶 α?(IC₅₀=440?μM) 和 DNA聚合酶?δ (IC₅₀>550?μM)。Delavirdine mesylate 是 HIV-1 病毒复制的抑制剂，可以用于艾滋病的相关研究。

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Delavirdine mesylate Chemical Structure

CAS No. : 147221-93-0

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥401	In-stock
5 mg	￥330	In-stock
10 mg	￥520	In-stock
50 mg	￥960	In-stock
100 mg	￥1750	In-stock
200 mg	￥2880	In-stock
500 mg		询价
1 g		询价

or 大包装询价

* Please select Quantity before adding items.

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MCE 顾客使用本产品发表的 3 篇科研文献

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HIV HIV-1 HIV-2

生物活性
纯度 & 产品资料
参考文献

生物活性

Delavirdine (U 90152) mesylate is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine mesylate selectively inhibits HIV-1 reverse transcriptase (RT) (IC₅₀=0.26?μM) over DNA polymerase?α?(IC₅₀=440 μM) and polymerase?δ (IC₅₀>550?μM). Delavirdine mesylate is an inhibitor of HIV-1 replication and can can be used for the study of AIDs^[1].

IC₅₀ & Target

HIV-1

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
CEM-SS	ED₅₀	0.06 μM Compound: delavirdine mesylate	Antiviral activity against HIV1 3B infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect after 6 days by MTS assay Antiviral activity against HIV1 3B infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect after 6 days by MTS assay	[PMID: 15217281]
MT4	EC₅₀	> 28.23 μM Compound: DLV	Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/YI81C double mutant infected in human MT4 cells assessed as cell viability after 4 days by MTT assay Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/YI81C double mutant infected in human MT4 cells assessed as cell viability after 4 days by MTT assay	[PMID: 26994843]
MT4	CC₅₀	> 36 μM Compound: DLV	Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay	[PMID: 25707013]
MT4	CC₅₀	> 36 μM Compound: DLV	Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability after 4 days by MTT assay	[PMID: 25626145]
MT4	EC₅₀	> 36 μM Compound: DLV	Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N/Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 25707013]
MT4	EC₅₀	> 36 μM Compound: DLV	Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N + Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N + Y181C double mutant infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 25626145]
MT4	CC₅₀	> 36 μM Compound: DLV	Cytotoxicity against human MT4 cells after 5 days by MTT assay Cytotoxicity against human MT4 cells after 5 days by MTT assay	[PMID: 24239481]
MT4	EC₅₀	> 36 μM Compound: DLV	Antiviral activity against drug-resistant HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT-4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay Antiviral activity against drug-resistant HIV1 RES056 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT-4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay	[PMID: 24239481]
MT4	CC₅₀	> 36.19 μM Compound: DLV	Cytotoxicity against human MT4 cells after 5 days by MTT assay Cytotoxicity against human MT4 cells after 5 days by MTT assay	[PMID: 22591854]
MT4	EC₅₀	> 36.19 μM Compound: DLV	Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV1 RES056 harboring reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 22591854]
MT4	CC₅₀	> 36.2 μM Compound: DLV	Cytotoxicity against human MT4 cells after 5 days by MTT assay Cytotoxicity against human MT4 cells after 5 days by MTT assay	[PMID: 22405288]
MT4	EC₅₀	> 36.2 μM Compound: DLV	Antiviral activity against HIV1 expressing reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay Antiviral activity against HIV1 expressing reverse transcriptase K103N/Y181C mutant infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay	[PMID: 22405288]
MT4	EC₅₀	> 43.81 μM Compound: DLV	Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N + Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay Antiviral activity against HIV1 RES056 expressing reverse transcriptase K103N + Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay	[PMID: 25240095]
MT4	CC₅₀	> 43.81 μM Compound: DLV	Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay	[PMID: 25240095]
MT4	EC₅₀	0.027 μM Compound: DLV	Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as cell viability after 4 days by MTT assay Antiviral activity against wild type HIV1 3B infected in human MT4 cells assessed as cell viability after 4 days by MTT assay	[PMID: 26994843]
MT4	EC₅₀	0.06 μM Compound: DLV (Mesylate)	Antiviral activity against HIV-1 3B harboring RT E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay Antiviral activity against HIV-1 3B harboring RT E138K mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay	[PMID: 21872971]
MT4	EC₅₀	0.13 μM Compound: DLV	Antiviral activity against HIV1 3B infected in human MT-4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay Antiviral activity against HIV1 3B infected in human MT-4 cells assessed as protection against virus-induced cytopathicity after 5 days by MTT assay	[PMID: 24239481]
MT4	EC₅₀	0.54 μM Compound: DLV	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 25707013]
MT4	EC₅₀	0.66 μM Compound: DLV	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay	[PMID: 25240095]
MT4	EC₅₀	1.72 μM Compound: DLV (Mesylate)	Antiviral activity against HIV-1 3B harboring RT K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay Antiviral activity against HIV-1 3B harboring RT K103N mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay	[PMID: 21872971]
MT4	EC₅₀	2.23 μM Compound: DLV (Mesylate)	Antiviral activity against HIV-1 3B harboring RT L100I mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay Antiviral activity against HIV-1 3B harboring RT L100I mutant infected in human MT4 cells assessed as inhibition of virus-induced syncytium formation after 5 days by MTT assay	[PMID: 21872971]
MT4	CC₅₀	28.23 μM Compound: DLV	Cytotoxicity against mock infected human MT4 cells after 4 days by MTT assay Cytotoxicity against mock infected human MT4 cells after 4 days by MTT assay	[PMID: 26994843]
MT4	CC₅₀	30.4 μM Compound: DLV	Cytotoxicity against human MT4 cells after 5 days by MTT assay Cytotoxicity against human MT4 cells after 5 days by MTT assay	[PMID: 28254696]
MT4	EC₅₀	32.6 nM Compound: DLV	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells assessed as protection against virus-induced cytotoxicity after 5 days by MTT assay	[PMID: 22405288]
MT4	EC₅₀	35.01 nM Compound: DLV	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 22591854]
MT4	EC₅₀	540 nM Compound: DLV	Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells assessed as reduction in virus-induced cytopathic effect after 5 days by MTT assay	[PMID: 25626145]

体外研究
(In Vitro)

在 H9 和 PBMC 培养物中，Delavirdine 在浓度 >100 μM 时具有 50% 的细胞毒性。Delavirdine 具有低细胞毒性，在 100 μM 时导致外周血淋巴细胞活力降低不到 8%^[1]。
Delavirdine 抑制 HIV-1 逆转录酶 (RT) 野生型，IC₅₀ 值为 0.26 μM，它抑制 Y181C 取代的 RT 和 K103N 取代的 RT，IC₅₀ 值分别为 8.32 uM 和 7.7 uM^[1]。

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

体内研究
(In Vivo)

Delavirdine (U 90152) mesylate (oral gavage；10 mg/kg，200 mg/kg，250 mg/kg；single dose) 吸收和代谢迅速，构成循环中的次要成分，其药代动力学呈非线性，并且在 CD-1 小鼠中其代谢为脱烷基地拉韦定的能力有限或可抑制 (PK 研究)^[1]。

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

Clinical Trial

分子量

552.67

Formula

C₂₃H₃₂N₆O₆S₂

CAS 号

147221-93-0

性状

固体

颜色

White to yellow

中文名称

地拉夫定甲磺酸盐；甲磺酸地拉韦啶

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 40.3 mg/mL (72.92 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8094 mL	9.0470 mL	18.0940 mL
5 mM	0.3619 mL	1.8094 mL	3.6188 mL
10 mM	0.1809 mL	0.9047 mL	1.8094 mL

查看完整储备液配制表

* 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

摩尔计算器
稀释计算器

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

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.52 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.52 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.52 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： 0.5% CMC-Na/saline water
Solubility: 5 mg/mL (9.05 mM); 悬浊液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.82%

选择批次：

Data Sheet (644 KB) SDS (252 KB)

COA (293 KB) LCMS (268 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Dueweke TJ, et al. U-90152, a potent inhibitor of human immunodeficiency virus type 1 replication. Antimicrob Agents Chemother. 1993 May;37(5):1127-31. [Content Brief]

[2]. Mayland Chang, et al. Metabolism of the HIV-1 Reverse Transcriptase Inhibitor Delavirdine In Mice. Research Article

Delavirdine mesylate 相关分类

Infection

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.8094 mL	9.0470 mL	18.0940 mL	45.2350 mL
	5 mM	0.3619 mL	1.8094 mL	3.6188 mL	9.0470 mL
	10 mM	0.1809 mL	0.9047 mL	1.8094 mL	4.5235 mL
	15 mM	0.1206 mL	0.6031 mL	1.2063 mL	3.0157 mL
	20 mM	0.0905 mL	0.4523 mL	0.9047 mL	2.2617 mL
	25 mM	0.0724 mL	0.3619 mL	0.7238 mL	1.8094 mL
	30 mM	0.0603 mL	0.3016 mL	0.6031 mL	1.5078 mL
	40 mM	0.0452 mL	0.2262 mL	0.4523 mL	1.1309 mL
	50 mM	0.0362 mL	0.1809 mL	0.3619 mL	0.9047 mL
	60 mM	0.0302 mL	0.1508 mL	0.3016 mL	0.7539 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:

Delavirdine147221-93-0U 90152BHAP-U 90152地拉夫定甲磺酸盐甲磺酸地拉韦啶U90152U-90152HIVReverse TranscriptaseHuman immunodeficiency virusNNRTIpolymeraseHIV-1 RTAIDsDLVInhibitorinhibitorinhibit

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Delavirdine mesylate (Synonyms: 地拉夫定甲磺酸盐; U 90152 mesylate; BHAP-U 90152 mesylate)

Customer Review

Other Forms of Delavirdine mesylate:

MCE 顾客使用本产品发表的 3 篇科研文献

Delavirdine mesylate 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 HIV 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

Delavirdine mesylate 相关分类

完整储备液配制表

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Delavirdine mesylate (Synonyms: 地拉夫定甲磺酸盐; U 90152 mesylate; BHAP-U 90152 mesylate)

Customer Review

Other Forms of Delavirdine mesylate:

Delavirdine mesylate 相关抗体

MCE 顾客使用本产品发表的 3 篇科研文献

Delavirdine mesylate 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 HIV 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

Delavirdine mesylate 相关抗体:

摩尔计算器

稀释计算器

Delavirdine mesylate 相关分类

完整储备液配制表

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您最近查看的产品:

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