Bosentan

• Description:

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

• UNSPSC:

  12352005

• Hazard Statement:

  H302, H361, H410

• Target:

  Endothelin Receptor

• Type:

  Reference compound

• Related Pathways:

  GPCR/G Protein

• Applications:

  COVID-19-immunoregulation

• Field of Research:

  Cardiovascular Disease; Endocrinology; Cancer

• Assay Protocol:

  https://www.medchemexpress.com/Bosentan.html

• Concentration:

  10mM

• Purity:

  99.98

• Solubility:

  DMSO : ≥ 100 mg/mL

• 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

• Molecular Formula:

  C27H29N5O6S

• Molecular Weight:

  551.61

• Precautions:

  H302, H361, H410

• References & Citations:

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

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Launched

• Citation 01:

  Acta Pharmacol Sin. 2023 May;44 (5) :984-998.|Am J Physiol Endocrinol Metab. 2019 Sep 1;317 (3) :E548-E558.|Am J Physiol Heart Circ Physiol. 2019 Nov 1;317 (5) :H1166-H1172.|Biomater Res. 2025 Nov 7:29:0280.|Biomater Res. 2025 Oct 22.|Biomed Pharmacother. 2025 Aug:189:118341.|Biopharm Drug Dispos. 2022 Dec;43 (6) :265-271.|bioRxiv. 2023 Apr 22.|Biotechnol Bioeng. 2021 Dec;118 (12) :4687-4698.|BMC Cancer. 2018 Feb 6;18 (1) :154.|Cell Biol Toxicol. 2021 Dec;37 (6) :873-890.|Cell Death Dis. 2024 May 22;15 (5) :358.|Cells. 2021 Nov 8;10 (11) :3072.|Chem Res Toxicol. 2025 Feb 17;38 (2) :281-295.|Clin Immunol. 2023 Sep:254:109687.|Curr Issues Mol Biol. 2023 Jan 8;45 (1) :555-570.|Department of Physiology and Pathophysiology. 2020 Sep.|Hypertension. 2019 Dec;74 (6) :1409-1419. |J Chromatogr B Analyt Technol Biomed Life Sci. 2025 Feb 1:1252:124443.|J Toxicol Sci. 2024;49 (8) :337-348.|Microcirculation. 2022 Oct;29 (6-7) :e12724.|Patent. US20220288064A1.|Patent. US20220317132A1.|Phytomedicine. 2019 Mar 15:56:175-182.|Phytomedicine. 2023 Dec:121:155054.|PLoS One. 2016 Dec 28;11 (12) :e0167713.|Sci Rep. 2022 Sep 28;12 (1) :16156.|Toxicology. 2020 May 15;437:152445.|Toxicology. 2025 Jun 3:154210.|J Exp Clin Cancer Res. 2025 Feb 21;44 (1) :64.

• CAS Number:

  147536-97-8