Bosentan (Synonyms: 波生坦)

目录号: HY-A0013 纯度: 99.98%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Bosentan 是一种有效的 endothelin-1 (ET) 拮抗剂，在人的 SMC 细胞中，作用于 ET_A 和 ET_B 受体，K_i 值分别为 4.7 nM 和 95 nM。

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Bosentan Chemical Structure

CAS No. : 147536-97-8

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥660	In-stock
50 mg	￥600	In-stock
100 mg	￥1050	In-stock
200 mg	￥2000	In-stock
500 mg	￥3078	In-stock
1 g		询价
5 g		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of Bosentan:

MCE 顾客使用本产品发表的 23 篇科研文献

: Bosentan purchased from MCE. Usage Cited in: Phytomedicine. 2019 Mar 15;56:175-182. [Abstract]; Representative Western blots for P-gp、BCRP、MRP2 in LS-180 treated with six active compounds in liquorice. C: control, P-1: Rifampicin, P-2: Bosentan, S-1: Liquiritin, S-2: Liquiritigenin, S-3: Isoliquiritin, S-4: Isoliquiritigenin, S-5: Glycyrrhetinic acid, S-6: Licochalcone A.

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ET_A ET_B

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ET_A and ET_B receptors with K_i of 4.7 nM and 95 nM in human SMC, respectively.

IC₅₀ & Target

Ki: 4.7 nM (ET_A receptor, in human SMC), 95 nM (ET_A receptor, in human SMC)^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A-375	IC₅₀	67.36 μM Compound: bosentan	Cytotoxicity against human A-375 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay Cytotoxicity against human A-375 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay	[PMID: 34473510]
B16	IC₅₀	> 80 μM Compound: bosentan	Cytotoxicity against mouse B16 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay Cytotoxicity against mouse B16 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay	[PMID: 34473510]
CHO	IC₅₀	202 nM Compound: 1	Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis	[PMID: 22862294]
CHO	IC₅₀	45 nM Compound: 1	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	[PMID: 22862294]
CHO-K1	IC₅₀	195.9 μM Compound: 1	Cytotoxicity against CHOK1 cells assessed as decrease in cell viability after 24 hrs by MTT assay Cytotoxicity against CHOK1 cells assessed as decrease in cell viability after 24 hrs by MTT assay	[PMID: 27318985]
HepG2	EC₅₀	12.6 μM Compound: Bosentan	Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis	[PMID: 20966043]
HepG2	EC₅₀	14.1 μM Compound: Bosentan	Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis	[PMID: 20966043]
SK-MEL-28	IC₅₀	53.65 μM Compound: bosentan	Cytotoxicity against human SK-MEL-28 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay Cytotoxicity against human SK-MEL-28 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay	[PMID: 34473510]

体外研究
(In Vitro)

Bosentan (BOS) competitively and specifically antagonizes binding of ¹²⁵I-labelled ET-1 to ET_A receptors on human smooth muscle cells (SMC) and ET_B receptors on human placenta cells. The in vitro binding affinity of Bosentan to ET_A receptors on human SMC is 4.7 nM and to ET_B receptors on human SMC or placenta cells is 41 or 95 nM. Bosentan has 67-fold greater selectivity for ET_A than ET_B receptors (mean IC₅₀=7.1 vs 474.8 nM) in an in vitro ¹²⁵I-labeling assay^[1].

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

体内研究
(In Vivo)

In hypertensive rats, Macitentan 30 mg/kg further decreases mean arterial blood pressure (MAP) by 19 mm Hg when given on top of Bosentan 100 mg/kg. Conversely, Bosentan given on top of Macitentan fails to induce an additional MAP decrease. In pulmonary hypertensive rats, Macitentan 30 mg/kg further decreases mean pulmonary artery pressure (MPAP) by 4 mm Hg on top of Bosentan, whereas a maximal effective dose of Bosentan given on top of Macitentan does not cause any additional MPAP decrease^[3].

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

Clinical Trial

分子量

551.61

Formula

C₂₇H₂₉N₅O₆S

CAS 号

147536-97-8

性状

固体

颜色

White to off-white

中文名称

伯森坦；柏森坦；波生坦

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	1 year
	-20°C	6 months

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 100 mg/mL (181.29 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	1.8129 mL	9.0644 mL	18.1287 mL
5 mM	0.3626 mL	1.8129 mL	3.6258 mL
10 mM	0.1813 mL	0.9064 mL	1.8129 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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6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： 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.75 mg/mL (4.99 mM); 澄清溶液
方案二

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.75 mg/mL (4.99 mM); 澄清溶液
方案三

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.53 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。
方案四

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.53 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。
方案五

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.53 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。

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: 99.98%

选择批次：

Data Sheet (633 KB) SDS (563 KB)

COA (200 KB) RP-HPLC (274 KB) LCMS (265 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Dhillon S, et al. Bosentan: a review of its use in the management of mildly symptomatic pulmonary arterial hypertension. Am J Cardiovasc Drugs. 2009;9(5):331-50. [Content Brief]

[2]. Akamata K, et al. Bosentan reverses the pro-fibrotic phenotype of systemic sclerosis dermal fibroblasts via increasing DNA binding ability of transcription factor Fli1. Arthritis Res Ther. 2014 Apr 3;16(2):R86. [Content Brief]

[3]. Iglarz M, et al. Comparison of pharmacological activity of macitentan and bosentan in preclinical models of systemic and pulmonary hypertension. Life Sci. 2014 Nov 24;118(2):333-9. [Content Brief]

[4]. Son GY, et al. Endothelin Regulates Porphyromonas gingivalis-Induced Production of Inflammatory Cytokines. PLoS One. 2016 Dec 28;11(12):e0167713. [Content Brief]

Cell Assay ^[2]	Cell viability is evaluated by the trypan blue exclusion test. Human dermal fibroblasts are treated with the indicated concentration of Bosentan (10, 20 and 40 μM). Cell viability is examined at 24 and 48 hours. Stained (dead) and unstained (viable) cells are counted with a hematocytometer^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	Rats^[3] Two-month-old DSS rats and two-month-old Wistar rats are used. Pharmacological effects on mean arterial pressure (MAP) or mean pulmonary arterial pressure (MPAP) and heart rate (HR) are measured up to 120 h after a single gavage at doses ranging from 0.1 to 100 mg/kg (Macitentan) or 3 to 600 mg/kg (Bosentan). To determine whether Macitentan can provide superior pharmacological activity vs. Bosentan, a study is designed in which: 1) Macitentan is administered on top of the maximal effective dose of Bosentan established by the dose-response curve. 2) the same dose of Bosentan is administered on top of the maximal effective dose of Macitentan. The maximal effective dose of the second compound is administered at T_max of the first tested compound. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Dhillon S, et al. Bosentan: a review of its use in the management of mildly symptomatic pulmonary arterial hypertension. Am J Cardiovasc Drugs. 2009;9(5):331-50. [Content Brief] [2]. Akamata K, et al. Bosentan reverses the pro-fibrotic phenotype of systemic sclerosis dermal fibroblasts via increasing DNA binding ability of transcription factor Fli1. Arthritis Res Ther. 2014 Apr 3;16(2):R86. [Content Brief] [3]. Iglarz M, et al. Comparison of pharmacological activity of macitentan and bosentan in preclinical models of systemic and pulmonary hypertension. Life Sci. 2014 Nov 24;118(2):333-9. [Content Brief] [4]. Son GY, et al. Endothelin Regulates Porphyromonas gingivalis-Induced Production of Inflammatory Cytokines. PLoS One. 2016 Dec 28;11(12):e0167713. [Content Brief]

Bosentan 相关分类

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	1.8129 mL	9.0644 mL	18.1288 mL	45.3219 mL
	5 mM	0.3626 mL	1.8129 mL	3.6258 mL	9.0644 mL
	10 mM	0.1813 mL	0.9064 mL	1.8129 mL	4.5322 mL
	15 mM	0.1209 mL	0.6043 mL	1.2086 mL	3.0215 mL
	20 mM	0.0906 mL	0.4532 mL	0.9064 mL	2.2661 mL
	25 mM	0.0725 mL	0.3626 mL	0.7252 mL	1.8129 mL
	30 mM	0.0604 mL	0.3021 mL	0.6043 mL	1.5107 mL
	40 mM	0.0453 mL	0.2266 mL	0.4532 mL	1.1330 mL
	50 mM	0.0363 mL	0.1813 mL	0.3626 mL	0.9064 mL
	60 mM	0.0302 mL	0.1511 mL	0.3021 mL	0.7554 mL
	80 mM	0.0227 mL	0.1133 mL	0.2266 mL	0.5665 mL
	100 mM	0.0181 mL	0.0906 mL	0.1813 mL	0.4532 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:

Bosentan147536-97-8伯森坦柏森坦波生坦Endothelin ReceptorInhibitorinhibitorinhibit

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Bosentan (Synonyms: 波生坦)

Customer Review

Other Forms of Bosentan:

MCE 顾客使用本产品发表的 23 篇科研文献

Bosentan 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Endothelin Receptor 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

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稀释计算器

Bosentan 相关分类

完整储备液配制表

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Bosentan (Synonyms: 波生坦)

Customer Review

Other Forms of Bosentan:

Bosentan 相关抗体

MCE 顾客使用本产品发表的 23 篇科研文献

Bosentan 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Endothelin Receptor 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

Bosentan 相关抗体:

摩尔计算器

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完整储备液配制表

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