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Bosentan (hydrate)

Catalog No. T6265   CAS 157212-55-0
Synonyms: Bosentan Hydrate, Benzenesulfonamide, Actelion, Ro 47-0203

Bosentan 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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Bosentan (hydrate) Chemical Structure
Bosentan (hydrate), CAS 157212-55-0
Pack Size Availability Price/USD Quantity
25 mg In stock $ 39.00
50 mg In stock $ 55.00
100 mg In stock $ 97.00
200 mg In stock $ 163.00
500 mg In stock $ 297.00
1 mL * 10 mM (in DMSO) In stock $ 61.00
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Purity: 99.75%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Bosentan 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.
Targets&IC50 ET-B:95 nM(Ki), ET-A:4.7 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]
Cell Research Bosentan 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].
Synonyms Bosentan Hydrate, Benzenesulfonamide, Actelion, Ro 47-0203
Molecular Weight 569.63
Formula C27H29N5O6S·H2O
CAS No. 157212-55-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 93 mg/mL (163.3 mM)

Ethanol: 2 mg/mL (3.51 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Ostrowski RP, et al. Pathophysiology, 2003, 9(4), 249-256. 2. Clozel M, et al. J Pharmacol Exp Ther, 1994, 270(1), 228-235.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Human Metabolite Library GPCR Compound Library Bioactive Compound Library Neurotransmitter Receptor Compound Library Clinical Compound Library Approved Drug Library FDA-Approved & Pharmacopeia Drug Library

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Keywords

Bosentan (hydrate) 157212-55-0 GPCR/G Protein Endothelin Receptor Bosentan Bosentan Hydrate inhibit Benzenesulfonamide Inhibitor Actelion Ro 47-0203 inhibitor

 

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