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Postion:Product Catalog >Biochemical Engineering>Inhibitors>GPCR & G Protein>Endothelin Receptor Antagonists>Bosentan (hydrate)
Bosentan (hydrate)
  • Bosentan (hydrate)

Bosentan (hydrate) NEW

Price $39 $55 $97
Package 25mg 50mg 100mg
Supply Ability: 10g
Update Time: 2026-06-02

Product Details

Product Name: Bosentan (hydrate) CAS No.: 157212-55-0
Purity: 99.31% Supply Ability: 10g
Release date: 2026/06/02

Product Introduction

Bioactivity

NameBosentan (hydrate)
DescriptionBosentan hydrate (Ro 47-0203) is a competitive and dual antagonist of endothelin-1 at the endothelin-A (ET-A) and endothelin-B (ET-B) receptors.
Cell ResearchBosentan is prepared in DMSO and diluted with appropriate medium before use[2]. Cell viability is evaluated by the trypan blue exclusion test. Human dermal fibroblasts are treated with the indicated concentration of Bosentan (10, 20 and 40 μM). Cell viability is examined at 24 and 48 hours. Stained (dead) and unstained (viable) cells are counted with a hematocytometer[2].
In vitroBosentan 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 vivoBosentan 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]
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
Solubility InformationDMSO : 250 mg/mL (438.88 mM), Sonication is recommended.
Ethanol : 2 mg/mL (3.51 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+90% Saline : < 10 mg/mL (17.56 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (17.56 mM), Solution.
KeywordsInhibitor | inhibit | ET-B | ET-A | EndothelinReceptor | Endothelin Receptor | Bosentan (hydrate) | Bosentan
Inhibitors RelatedBQ-788 | Macitentan | BMS 182874 | Bosentan | BMS 182874 hydrochloride | Sitaxsentan sodium | Edonentan | SB-209670 | Ambrisentan | Sparsentan | Aprocitentan | Clazosentan
Related Compound LibrariesFailed Clinical Trials Compound Library | Bioactive Compound Library | Pain-Related Compound Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | FDA-Approved Drug Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | GPCR Compound Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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TargetMol Chemicals Inc.

6YR United StatesUnited States
  • Since: 2011-01-07
  • Address: 36 Washington Street, Wellesley Hill, MA
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