Temsavir (Synonyms: BMS-626529)

目录号: HY-15440 纯度: 98.06%: FAQs
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Temsavir (BMS-626529) 是一种 HIV-1 gp120 抑制剂，抑制其结合到 CD4⁺ T 细胞。

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Temsavir Chemical Structure

CAS No. : 701213-36-7

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥675	In-stock
1 mg	￥244	In-stock
5 mg	￥648	In-stock
10 mg	￥1035	In-stock
25 mg	￥1850	In-stock
50 mg	￥2838	In-stock
100 mg	￥4100	In-stock
200 mg		询价
500 mg		询价

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Customer Review

Other Forms of Temsavir:

Fostemsavir In-stock
Fostemsavir Tris In-stock

MCE 顾客使用本产品发表的 4 篇科研文献

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HIV HIV-1 HIV-2

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Temsavir (BMS-626529) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4⁺ T cells.

IC₅₀ & Target

HIV-1

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
HCT-116	CC₅₀	> 200 μM Compound: 31; BMS-626529	Cytotoxicity against human HCT116 cells after 6 days by XTT assay Cytotoxicity against human HCT116 cells after 6 days by XTT assay	[PMID: 29271653]
HEK293	CC₅₀	> 200 μM Compound: 31; BMS-626529	Cytotoxicity against HEK293 cells after 6 days by XTT assay Cytotoxicity against HEK293 cells after 6 days by XTT assay	[PMID: 29271653]
HeLa	CC₅₀	> 200 μM Compound: 31; BMS-626529	Cytotoxicity against human HeLa cells after 6 days by XTT assay Cytotoxicity against human HeLa cells after 6 days by XTT assay	[PMID: 29271653]
HeLa	CC₅₀	> 300 μM Compound: 1; BMS-626529	Cytotoxicity against human HeLa cells after 6 days by MTT assay Cytotoxicity against human HeLa cells after 6 days by MTT assay	[PMID: 26584882]
HEp-2	CC₅₀	> 200 μM Compound: 31; BMS-626529	Cytotoxicity against human Hep2 cells after 6 days by XTT assay Cytotoxicity against human Hep2 cells after 6 days by XTT assay	[PMID: 29271653]
HepG2	CC₅₀	> 200 μM Compound: 31; BMS-626529	Cytotoxicity against human HepG2 cells after 6 days by XTT assay Cytotoxicity against human HepG2 cells after 6 days by XTT assay	[PMID: 29271653]
HOS	CC₅₀	> 200 μM Compound: 31; BMS-626529	Cytotoxicity against HOS cells after 6 days by XTT assay Cytotoxicity against HOS cells after 6 days by XTT assay	[PMID: 29271653]
MCF7	CC₅₀	> 200 μM Compound: 31; BMS-626529	Cytotoxicity against human MCF7 cells after 6 days by XTT assay Cytotoxicity against human MCF7 cells after 6 days by XTT assay	[PMID: 29271653]
MT2	CC₅₀	> 200 μM Compound: 31; BMS-626529	Cytotoxicity against human MT2 cells after 6 days by XTT assay Cytotoxicity against human MT2 cells after 6 days by XTT assay	[PMID: 29271653]
MT2	CC₅₀	> 300 μM Compound: 3; BMS-626529	Cytotoxicity against human MT2 cells assessed as decrease in cell viability after 3 days by XTT assay Cytotoxicity against human MT2 cells assessed as decrease in cell viability after 3 days by XTT assay	[PMID: 29920093]
MT2	EC₅₀	0.7 nM Compound: 12a	Antiviral activity against CXCR4-tropic HIV1 LAI infected in human MT2 cells by monogram phenosense entry assay Antiviral activity against CXCR4-tropic HIV1 LAI infected in human MT2 cells by monogram phenosense entry assay	[PMID: 26116177]
MT2	EC₅₀	14.8 nM Compound: 12a	Antiviral activity against CXCR4-tropic HIV1 MN infected in human MT2 cells by monogram phenosense entry assay Antiviral activity against CXCR4-tropic HIV1 MN infected in human MT2 cells by monogram phenosense entry assay	[PMID: 26116177]
MT2	EC₅₀	16.2 nM Compound: 12a	Antiviral activity against CXCR4-tropic HIV1 3B infected in human MT2 cells by monogram phenosense entry assay Antiviral activity against CXCR4-tropic HIV1 3B infected in human MT2 cells by monogram phenosense entry assay	[PMID: 26116177]
MT2	EC₅₀	2.2 nM Compound: 12a	Antiviral activity against CXCR4-tropic HIV1 NL4-3 infected in human MT2 cells by monogram phenosense entry assay Antiviral activity against CXCR4-tropic HIV1 NL4-3 infected in human MT2 cells by monogram phenosense entry assay	[PMID: 26116177]
NCI-H292	CC₅₀	> 200 μM Compound: 31; BMS-626529	Cytotoxicity against human NCI-H292 cells after 6 days by XTT assay Cytotoxicity against human NCI-H292 cells after 6 days by XTT assay	[PMID: 29271653]
PBMC	CC₅₀	> 10 μM Compound: BMS-626529	Cytotoxicity against human PBMC cells assessed as reduction in cell viability incubated for 1 hr followed by complete medium addition and measured after 48 hrs by XTT assay Cytotoxicity against human PBMC cells assessed as reduction in cell viability incubated for 1 hr followed by complete medium addition and measured after 48 hrs by XTT assay	[PMID: 29860061]
PBMC	CC₅₀	192 μM Compound: 31; BMS-626529	Cytotoxicity against human PBMC after 6 days by XTT assay Cytotoxicity against human PBMC after 6 days by XTT assay	[PMID: 29271653]
SK-N-MC	CC₅₀	> 200 μM Compound: 31; BMS-626529	Cytotoxicity against human SK-N-MC cells after 6 days by XTT assay Cytotoxicity against human SK-N-MC cells after 6 days by XTT assay	[PMID: 29271653]
TZM	CC₅₀	> 100 μM Compound: BMS-626529	Cytotoxicity against human TZM-bl cells incubated for 3 days by MTS assay Cytotoxicity against human TZM-bl cells incubated for 3 days by MTS assay	[PMID: 32031803]

体外研究
(In Vitro)

Temsavir 对绝大多数病毒分离株的半数最大有效浓度 (EC₅₀) 值 <10 nM。Temsavir 对 LAI 病毒的平均 EC₅₀ 为 0.7±0.4 nM。Temsavir 对最易感病毒的 EC₅₀ 为 0.01 nM，对最不敏感的病毒的 EC₅₀ >2，000 nM。Temsavir 的细胞毒性特征在来自不同人体组织的几种细胞类型中进行了检查。在 MT-2 (T 淋巴细胞)、HEK293 (肾脏)、HEp-2 (喉)、HepG2 (肝脏)、HeLa (子宫颈)、HCT116 (结直肠癌) 中观察到 CC₅₀ 值 >200 μM)、MCF-7 (乳腺)、SK-N-MC (神经上皮细胞)、HOS (骨)、H292 (肺) 和 MDBK (牛肾) 细胞在培养 3 或 6 天后测量。在培养 6 天后，T 细胞系 PM1 和 PBMC 中的 CC₅₀ 值分别为 105 和 192 μM。这些结果表明，Temsavir 在细胞培养中表现出低细胞毒性^[1]。Temsavir 对一组临床分离株表现出广谱抗病毒活性，其 50% 抑制浓度 (IC₅₀) 范围从亚纳摩尔水平到 >0.1 μM^[2] .

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

Clinical Trial

分子量

473.48

Formula

C₂₄H₂₃N₇O₄

CAS 号

701213-36-7

性状

固体

颜色

White to off-white

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
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 16.67 mg/mL (35.21 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	2.1120 mL	10.5601 mL	21.1202 mL
5 mM	0.4224 mL	2.1120 mL	4.2240 mL
10 mM	0.2112 mL	1.0560 mL	2.1120 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

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: ≥ 1.67 mg/mL (3.53 mM); 澄清溶液

此方案可获得 ≥ 1.67 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 16.7 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: ≥ 1.67 mg/mL (3.53 mM); 澄清溶液

此方案可获得 ≥ 1.67 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 16.7 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: ≥ 1.67 mg/mL (3.53 mM); 澄清溶液

此方案可获得 ≥ 1.67 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 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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）。

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: 98.06%

选择批次：

Data Sheet (650 KB) SDS (583 KB)

COA (294 KB) LCMS (87 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Nowicka-Sans B, et al. In vitro antiviral characteristics of HIV-1 attachment inhibitor BMS-626529, the active component of the prodrug BMS-663068. Antimicrobial Agents and Chemotherapy (2012), 56(7), 3498-3507. [Content Brief]

[2]. Nettles RE, et al. Pharmacodynamics, safety, and pharmacokinetics of BMS-663068, an oral HIV-1 attachment inhibitor in HIV-1-infected subjects. J Infect Dis. 2012 Oct 1;206(7):1002-11. [Content Brief]

Kinase Assay ^[1]	Micro BioSpin 6 columns are used to measure the binding of [³H]BMS-488043 or [³H]Temsavir to gp120. Binding solutions (30 μL) containing 25 mM Tris-HCl (pH 7.5), 125 mM NaCl, 50 nM gp120_JRFL, and serial dilutions of [³H]BMS-488043 or [³H]Temsavir are allowed to equilibrate and then adsorbed to a MicroBioSpin 6 column. The column is centrifuged (~14,000 rpm) for 5 min, the eluent is collected, and radioactivity is determined with a scintillation counter. To measure dissociative kinetics, 150 nM [³H]Temsavir or 90 nM [³H]BMS-488043 is incubated with 60 nM gp120 at ambient temperature for 1 h to achieve equilibrium binding, and then a large molar excess (14-fold) of soluble CD4 protein is added to drive dissociation. Aliquots are taken at the indicated time intervals, adsorbed to a spin column, and centrifuged, and the radioactivity in the eluent is quantitated. Comparison of the tritium signal from parallel samples with and without the soluble CD4 challenge allowed for the determination of the percent compound bound^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Cytotoxicity assays are performed in the presence of serially diluted Temsavir for up to 6 days, and cell viability is quantitated using an XTT assay. To determine CC₅₀ values (concentration of drug required to kill 50% of cells), laboratory-adapted peripheral blood mononuclear cells (PBMCs) are initially plated at a density of 0.1×10⁶ cells/mL. In the absence of compounds, the cell densities typically reach 1×10⁶ to 1.2×10⁶/mL after 6 days^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Nowicka-Sans B, et al. In vitro antiviral characteristics of HIV-1 attachment inhibitor BMS-626529, the active component of the prodrug BMS-663068. Antimicrobial Agents and Chemotherapy (2012), 56(7), 3498-3507. [Content Brief] [2]. Nettles RE, et al. Pharmacodynamics, safety, and pharmacokinetics of BMS-663068, an oral HIV-1 attachment inhibitor in HIV-1-infected subjects. J Infect Dis. 2012 Oct 1;206(7):1002-11. [Content Brief]

Temsavir 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	2.1120 mL	10.5601 mL	21.1202 mL	52.8005 mL
	5 mM	0.4224 mL	2.1120 mL	4.2240 mL	10.5601 mL
	10 mM	0.2112 mL	1.0560 mL	2.1120 mL	5.2801 mL
	15 mM	0.1408 mL	0.7040 mL	1.4080 mL	3.5200 mL
	20 mM	0.1056 mL	0.5280 mL	1.0560 mL	2.6400 mL
	25 mM	0.0845 mL	0.4224 mL	0.8448 mL	2.1120 mL
	30 mM	0.0704 mL	0.3520 mL	0.7040 mL	1.7600 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:

Temsavir701213-36-7BMS-626529BMS626529BMS 626529HIVHuman immunodeficiency virusInhibitorinhibitorinhibit

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Temsavir (Synonyms: BMS-626529)

Customer Review

Other Forms of Temsavir:

Temsavir 相关抗体

MCE 顾客使用本产品发表的 4 篇科研文献

Temsavir 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

实验参考方法

纯度 & 产品资料

参考文献

Temsavir 相关抗体:

摩尔计算器

稀释计算器

Temsavir 相关分类

完整储备液配制表

Keywords:

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