Bosentan

• UNSPSC 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.

• Target Antigen:

  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

• 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 Weight:

  551.61

• 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)

• Clinical Information:

  Launched

• CAS Number:

  147536-97-8