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Bosentan (hydrate)

Catalog No. T6265 CAS 157212-55-0

Synonyms: Bosentan Hydrate, Actelion, Benzenesulfonamide, Ro 47-0203

Bosentan is a competitive and dual antagonist of endothelin-1 at the endothelin-A (ET-A) and endothelin-B (ET-B) receptors.

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Bosentan (hydrate), CAS 157212-55-0

Pack Size	Availability	Price/USD
25 mg	In stock	$ 50.00
50 mg	In stock	$ 64.00
100 mg	In stock	$ 108.00
200 mg	In stock	$ 178.00
500 mg	In stock	$ 324.00
1 mL * 10 mM (in DMSO)	In stock	$ 64.00

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Purity: 99.75%

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Description	Bosentan 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, Actelion, Benzenesulfonamide, Ro 47-0203
Molecular Weight	569.63
Formula	C27H31N5O7S
CAS No.	157212-55-0

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 93 mg/mL (163.3 mM)

Ethanol: 2 mg/mL (3.51 mM)

H2O: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References 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-Cardiovascular Disease Compound Library Inhibitor Library FDA-Approved Drug Library NO PAINS Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Compound Library Endocrinology-Hormone Compound Library Neurotransmitter Receptor Compound Library Bioactive Compounds Library Max Anti-Hypertension Compound Library

Related Products

Related compounds with same targets

Avosentan Atrasentan hydrochloride Carperitide acetate Myriceric acid C BQ-123 Bosentan Darusentan BMS 182874 hydrochloride

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Keywords

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

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