Catalog No.S3051 Synonyms: Ro 47-0203
Molecular Weight(MW): 569.63
Bosentan is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively.
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|Description||Bosentan is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively.|
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. 
|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. 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. |
|In vitro||DMSO||100 mg/mL (175.55 mM)|
|Ethanol||2 mg/mL (3.51 mM)|
|Water||0.001 mg/mL (0.0 mM)|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02798055||Not yet recruiting||Systematic Sclerosis|Digital Ulcer|Scleroderma||Elpen Pharmaceutical Co. Inc.||June 2016||--|
|NCT02667704||Completed||Healthy||Boehringer Ingelheim||February 2016||Phase 1|
|NCT02480335||Not yet recruiting||Scleroderma, Systemic||University Medical Center Groningen|Actelion||June 2015||Phase 4|
|NCT02116335||Recruiting||Hypertension||Georgia Regents University|National Heart, Lung, and Blood Institute (NHLBI)||June 2015||--|
|NCT02377271||Not yet recruiting||Ischemic Optic Neuropathy||University Hospital, Grenoble||March 2015||Phase 3|
|NCT02389426||Completed||Multiple Sclerosis||Universitair Ziekenhuis Brussel||December 2014||--|
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