Art. -Nr.: HY-A0013A

Bosentan hydrate

32 Cited Publications

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Based on 32 publication(s) in Google Scholar

Bosentan hydrate 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.

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Reinheit: 99.93%
CAS. Nr.: 157212-55-0
Formel: C₂₇H₃₁N₅O₇S
Molecular Weight:569.63

Speicherung:

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

Bosentan hydrate Chemical Structure

CAS. Nr.: 157212-55-0

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (32)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

Bosentan hydrate 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]

Alle Endothelin Receptor Isoform-spezifische Produkte anzeigen :

ET_A
ET_B

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 hydrate 100 mg/kg. Conversely, Bosentan hydrate 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 hydrate, whereas a maximal effective dose of Bosentan hydrate 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.

Chemical Information

CAS. Nr. 157212-55-0
Appearance Solid
Molecular Weight 569.63
Formel C₂₇H₃₁N₅O₇S
Color Off-white to light yellow
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.O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (32)

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Journal Impact Factor

J Exp Clin Cancer Res

The extracellular matrix protein type I collagen and fibronectin are regulated by β-arrestin-1/endothelin axis in human ovarian fibroblasts. [Abstract]

2025 Feb 21;44(1):64. PMID: 39985042
Biomater Res

Distinct Roles of Matrigel Enabled the Production of Expandable Hepatoblast and Polarized Hepatocyte Organoids from Human Embryonic Stem Cells under 3-Dimensional Suspension Conditions. [Abstract]

2025 Nov 7:29:0280. PMID: 41209312
Cell Death Dis

The β-arrestin1/endothelin axis bolsters ovarian fibroblast-dependent invadosome activity and cancer cell metastatic potential. [Abstract]

2024 May 22;15(5):358. PMID: 38777849

Bosentan hydrate 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 hydrate 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 hydrate 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 hydrate 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 hydrate 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.
Acta Pharmacol Sin

Circulating small extracellular vesicles promote proliferation and migration of vascular smooth muscle cells via AXL and MerTK activation. [Abstract]

2023 May;44(5):984-998. PMID: 36450791
Phytomedicine

Celastrol as an intestinal FXR inhibitor triggers tripolide-induced intestinal bleeding: Underlying mechanism of gastrointestinal injury induced by Tripterygium wilfordii. [Abstract]

2023 Dec:121:155054. PMID: 37738906
Phytomedicine

Potential detoxification effect of active ingredients in liquorice by upregulating efflux transporter. [Abstract]

2019 Mar 15:56:175-182. PMID: 30668338

Bosentan hydrate 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.
Hypertension

Chronic Elevation of Endothelin-1 Alone May Not Be Sufficient to Impair Endothelium-Dependent Relaxation. [Abstract]

2019 Dec;74(6):1409-1419. PMID: 31630572
Biomed Pharmacother

GKB202 suppresses endothelin-1/ERK signaling in pancreatic cancer cells: Potential implications for circulating tumor cell regulation. [Abstract]

2025 Aug:189:118341. PMID: 40669304
Cell Biol Toxicol

Endothelial ERG alleviates cardiac fibrosis via blocking endothelin-1-dependent paracrine mechanism. [Abstract]

2021 Dec;37(6):873-890. PMID: 33469864
Biochem Pharmacol

Bosentan confers cardioprotection against cisplatin toxicity: Involvement of β-arrestin-linked ETA receptor signaling. [Abstract]

2026 Aug;250(Pt 2):118027. PMID: 42069228
Cells

The Endothelin Receptor Antagonist Macitentan Inhibits Human Cytomegalovirus Infection. [Abstract]

2021 Nov 8;10(11):3072. PMID: 34831300
Am J Physiol Cell Physiol

Redox-sensitive GPCR signaling drives Gq-dependent Ca²⁺ mobilization and cytokine production in human bronchial epithelial cells. [Abstract]

2026 Jun 18. PMID: 42314770
Eur J Pharmacol

tRF-31-PS5P4PW3FJHP inhibits hypoxia-induced proliferation of pulmonary artery endothelial cells by regulating EDN1 splicing via binding to LSM4. [Abstract]

2026 Jan 12:1011:178426. PMID: 41354297
Toxicology

In vitro test battery for testing molecular initiating events in chemical-induced cholestasis. [Abstract]

2025 Jun 3:154210. PMID: 40473197
Toxicology

Drug interaction study of flavonoids toward OATP1B1 and their 3D structure activity relationship analysis for predicting hepatoprotective effects. [Abstract]

2020 May 15;437:152445. PMID: 32259555
Am J Physiol Heart Circ Physiol

Persistent insulin signaling coupled with restricted PI3K activation causes insulin-induced vasoconstriction. [Abstract]

2019 Nov 1;317(5):H1166-H1172. PMID: 31603345
Sci Rep

Involvement of endothelins in neuroprotection of valosin-containing protein modulators against retinal ganglion cell damage. [Abstract]

2022 Sep 28;12(1):16156. PMID: 36171250
Chem Res Toxicol

Inhibitory Effects of Alkaloids on OATP1B1 In Vitro and In Vivo: Prediction for Food/Herb-Drug Interactions and Hepatoprotective Effects Based on Structure-Activity Relationships. [Abstract]

2025 Feb 17;38(2):281-295. PMID: 39899883
Clin Immunol

NETosis promotes chronic inflammation and fibrosis in systemic lupus erythematosus and COVID-19. [Abstract]

2023 Sep:254:109687. PMID: 37419296
Biotechnol Bioeng

An integrated biomimetic array chip for establishment of collagen-based 3D primary human hepatocyte model for prediction of clinical drug-induced liver injury. [Abstract]

2021 Dec;118(12):4687-4698. PMID: 34478150
BMC Cancer

Overexpression of endothelin B receptor in glioblastoma: a prognostic marker and therapeutic target?. [Abstract]

2018 Feb 6;18(1):154. PMID: 29409474
Am J Physiol Endocrinol Metab

Overproduction of endothelin-1 impairs glucose tolerance but does not promote visceral adipose tissue inflammation or limit metabolic adaptations to exercise. [Abstract]

2019 Sep 1;317(3):E548-E558. PMID: 31310581
Curr Issues Mol Biol

Deciphering the Mechanism of Wogonin, a Natural Flavonoid, on the Proliferation of Pulmonary Arterial Smooth Muscle Cells by Integrating Network Pharmacology and In Vitro Validation. [Abstract]

2023 Jan 8;45(1):555-570. PMID: 36661523
J Chromatogr B Analyt Technol Biomed Life Sci

A simple HPLC-UV method for monitoring therapeutic adherence in pulmonary arterial hypertension. [Abstract]

2025 Feb 1:1252:124443. PMID: 39787725
PLoS One

Endothelin Regulates Porphyromonas gingivalis-Induced Production of Inflammatory Cytokines. [Abstract]

2016 Dec 28;11(12):e0167713. PMID: 28030574
Biopharm Drug Dispos

Inhibition of canalicular and sinusoidal taurocholate efflux by cholestatic drugs in human hepatoma HepaRG cells. [Abstract]

2022 Dec;43(6):265-271. PMID: 36195987
Microcirculation

Lymphatic microcirculation profile in the progression of hypertension in spontaneously hypertensive rats. [Abstract]

2022 Oct;29(6-7):e12724. PMID: 34351675
J Toxicol Sci

Validation of a new protocol for a zebrafish MEFL (malformation or embryo-fetal lethality) test method that conforms to the ICH S5 (R3) guideline. [Abstract]

2024;49(8):337-348. PMID: 39098043
bioRxiv

2023 Apr 22.
Patent

US20220317132A1.
Patent

US20220288064A1.
University of Manitoba

2020 Sep.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (175.55 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 50 mg/mL (87.78 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7555 mL

8.7776 mL

17.5553 mL

5 mM

0.3511 mL

1.7555 mL

3.5111 mL

10 mM

0.1756 mL

0.8778 mL

1.7555 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass

Konzentration

Volumen

Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline