Bosentan

Name: Bosentan
Brand: MedChemExpress
SKU: HY-A0013
Rating: 5.0 (30 reviews)

Cat. No.: HY-A0013 Purity: 99.94%: Data Sheet
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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.

For research use only. We do not sell to patients.

CAS No. : 147536-97-8

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 30 publication(s) in Google Scholar

Other Forms of Bosentan:

Bosentan-d4 In-stock
Bosentan hydrate In-stock

30 Publications Citing Use of MCE Bosentan

Cell Imaging/Staining

In Vivo Efficacy Study

: Bosentan purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2024 May 22;15(5):358. [Abstract]; Bosentan (BOS) (1 μM; 5 min) abolished the increased HOF invasive potential induced by ET-1.

: Bosentan purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2024 May 22;15(5):358. [Abstract]; Bosentan (BOS) (1 μM; 5 min) inhibited the enhanced average invasion depth into the ECM of Kuramochi cells and HOFs induced by ET-1.

: Bosentan purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2024 May 22;15(5):358. [Abstract]; Bosentan (BOS) (10 mg/kg; i.p.; once daily for 5 weeks) significantly inhibited intraperitoneal spreading of tumors in NOD/SCID mice.

: Bosentan purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2024 May 22;15(5):358. [Abstract]; Bosentan (BOS) (10 mg/kg; i.p.; once daily for 5 weeks) markedly reduced the expression of PDGFR and Vimentin in metastatic nodules of NOD/SCID mice.

: Bosentan purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2024 May 22;15(5):358. [Abstract]; Bosentan (BOS) (10 mg/kg; i.p.; once daily for 5 weeks) significantly enhanced the number of apoptotic cells in the tumors of NOD/SCID mice.

: Bosentan purchased from MedChemExpress. 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

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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]

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	280 nM Compound: Bosentan 1	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETB receptor	[PMID: 12617929]
CHO	IC₅₀	40 nM Compound: Bosentan 1	In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor In vitro inhibitory concentration required against [125I]ET1 binding to membranes of CHO cells expressing human ETA receptor	[PMID: 12617929]
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	IC₅₀	8 nM Compound: 1a	Receptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cells Receptor binding affinity was determined in a radioligand binding assay against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected CHO cells	10.1016/S0960-894X(97)00400-9
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]
CHO-K1	IC₅₀	8.4 nM Compound: Bosentan	Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes Displacement of 125I-labelled endothelin-1 from human ETA receptor expressed in CHOK1 cell membranes	10.1039/C5MD00169B
CHO-K1	IC₅₀	8.9 nM Compound: Bosentan	Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells	[PMID: 22750010]
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]
Sf21	IC₅₀	30.6 μM Compound: Bosentan	Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	[PMID: 21965623]
Sf21	IC₅₀	38.1 μM Compound: Bosentan	Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	[PMID: 21965623]
Sf9	IC₅₀	0.08 μM Compound: 6	Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes	[PMID: 27321813]
Sf9	IC₅₀	80 nM Compound: 1a	Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells	10.1016/S0960-894X(97)00400-9

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].

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

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].

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

Clinical Trial

Molecular Weight

551.61

Formula

C₂₇H₂₉N₅O₆S

CAS No.

147536-97-8

Appearance

Solid

Color

White to off-white

SMILES

O=S(NC1=NC(C2=NC=CC=N2)=NC(OCCO)=C1OC3=CC=CC=C3OC)(C4=CC=C(C(C)(C)C)C=C4)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (181.29 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.75 mg/mL (4.99 mM); Clear solution
Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.75 mg/mL (4.99 mM); Clear solution
Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 4

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 2.5 mg/mL (4.53 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.94%

Select Batch:

Data Sheet (284 KB) SDS (623 KB)

COA (255 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[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.
References	[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

Bosentan Related Classifications

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:

Bosentan147536-97-8Endothelin ReceptorInhibitorinhibitorinhibit

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Bosentan

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Other Forms of Bosentan:

Bosentan Related Antibodies

30 Publications Citing Use of MCE Bosentan

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View All Endothelin Receptor Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Bosentan Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Bosentan Related Classifications

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