Home GPCR & G Protein Endothelin Receptor antagonist Bosentan Hydrate For research use only.

Bosentan Hydrate

Synonyms: Ro 47-0203

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.

Bosentan Hydrate Chemical Structure

Bosentan Hydrate Chemical Structure

CAS: 157212-55-0

Selleck's Bosentan Hydrate has been cited by 11 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

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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.
Targets
ET-A [1] ET-B [1]
4.7 nM(Ki) 95 nM(Ki)
In vitro
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
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 Animal Models Male Wistar rats with CHF
Dosages 100 mg/kg, 30 mg/kg
Administration Oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05072106 Unknown status Advanced Solid Tumor PharmaMar January 14 2021 Phase 1
NCT04991207 Completed Pulmonary Arterial Hypertension Bial - Portela C S.A. February 6 2018 Phase 1
NCT01929213 Unknown status Healthy Volunteers Dong-A Pharmaceutical Co. Ltd.|Dong-A ST Co. Ltd. August 2013 Phase 1

Chemical lnformation & Solubility

Molecular Weight 569.63 Formula

C27H29N5O6S.H2O
CAS No. 157212-55-0 SDF Download Bosentan Hydrate SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (175.55 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : 0.001 mg/mL


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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