Bosentan Hydrate

Catalog No.S3051 Synonyms: Ro 47-0203

Bosentan Hydrate Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 90 In stock
USD 70 In stock
USD 970 In stock

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Bosentan is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively.
Targets
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]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Male Wistar rats with CHF
  • Formulation: 5% gum arabic and prepared freshly every day
  • 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

* 1 mg/ml means slightly soluble or insoluble.
* 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
Formula

C27H29N5O6S.H2O

CAS No. 157212-55-0
Storage powder
in solvent
Synonyms Ro 47-0203

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03053739 Recruiting Associated Pulmonary Arterial Hypertension Postgraduate Institute of Medical Education and Research December 2016 Phase 4
NCT02798055 Not yet recruiting Systematic Sclerosis|Digital Ulcer|Scleroderma Elpen Pharmaceutical Co. Inc. September 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 Augusta University|National Heart, Lung, and Blood Institute (NHLBI) June 2015 --
NCT02377271 Not yet recruiting Ischemic Optic Neuropathy University Hospital, Grenoble March 2015 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