Bosentan Hydrate

For research use only.

Catalog No.S3051 Synonyms: Ro 47-0203

9 publications

Bosentan Hydrate Chemical Structure

CAS No. 157212-55-0

Bosentan (Ro 47-0203) is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively.

Selleck's Bosentan Hydrate has been cited by 9 publications

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Biological Activity

Description Bosentan (Ro 47-0203) is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively.
ET-A [1] ET-B [1]
4.7 nM(Ki) 95 nM(Ki)
In vitro

Bosentan competitively antagonizes the specific binding of [125 I]-labeled ET-1 on human smooth muscle cells (ET-A receptors)human placenta (ET-B receptors). Bosentan also inhibits the binding of selective ET-B ligands on porcine trachea. Contractions induced by ET-1 in isolated rat aorta (ET-A) and by the selective ET-B agonist sarafotoxin S6C in rat trachea are competitively inhibited by Bosentan (pA2= 7.2 and 6.0, respectively), as is the endothelium-dependent relaxation to sarafotoxin S6C in rabbit superior mesenteric artery (pA2= 6.7). The binding of 40 other peptides, prostaglandins, ions and neurotransmitters is not significantly affected by Bosentan, which shows its specificity for ET receptors. [1]

In vivo Bosentan inhibits the presser response to big ET-1 both after i.v. and oral administration, with a long duration of action and no intrinsic agonist activity. Bosentan also inhibits the depressor and presser effect of ET-1 and sarafotoxin S6C. Its pharmacological profile makes Bosentan a potentially useful drug in the management of clinical disorders associated with vasoconstriction.[1] Bosentan is the first oral non-peptide mixed ETA/B-receptor antagonist. Long-term treatment with Bosentan has markedly increased the survival, hemodynamics, and cardiac remodeling in rats with CHF. Bosentan decreases arterial BP to a similar degree as an angiotensin-converting enzyme (ACE) inhibitor. Administration of Bosentan in rats with CHF after acute MI significantly decreases arterial BP and has additive effect to that of an ACE inhibitor. Acute and chronical treatment with Bosentan also improves the systemic and pulmonary hemodynamics by a decrease in peripheral and pulmonary vascular resistance, and increase of cardiac output in patients with CHF. [2]


Animal Research:[1]
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  • Animal Models: Male Wistar rats with CHF
  • Dosages: 100 mg/kg, 30 mg/kg
  • Administration: Oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (175.55 mM)
Ethanol 2 mg/mL (3.51 mM)
Water 0.001 mg/mL (0.0 mM)
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 569.63


CAS No. 157212-55-0
Storage powder
in solvent
Synonyms Ro 47-0203
Smiles CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)NC2=C(C(=NC(=N2)C3=NC=CC=N3)OCCO)OC4=CC=CC=C4OC.O

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Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
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% DMSO % % Tween 80 % ddH2O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04991207 Completed Drug: BIA 5-1058|Drug: bosentan Pulmonary Arterial Hypertension Bial - Portela C S.A. February 6 2018 Phase 1
NCT01929213 Unknown status Drug: Udenafil|Drug: Bosentan|Drug: Udenafil/Bosentan Healthy Volunteers Dong-A Pharmaceutical Co. Ltd.|Dong-A ST Co. Ltd. August 2013 Phase 1
NCT01389856 Terminated Drug: Bosentan|Drug: Matching placebo Persistent Pulmonary Hypertension of the Newborn Actelion December 2011 Phase 3

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Endothelin Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID