[CAS NO. 157212-55-0] Bosentan Hydrate

Name: Bosentan Hydrate
Brand: Arctom Scientific
SKU: SLK-S3051

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PRODUCTS SPECIFICATIONS [157212-55-0]

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Catalog

SLK-S3051

Brand

Selleck

CAS

157212-55-0

DESCRIPTION [157212-55-0]

Overview

MDL	MFCD09751188
Molecular Weight	569.63
Molecular Formula	C27H29N5O6S.H2O
SMILES	O(C=1C(NS(=O)(=O)C2=CC=C(C(C)(C)C)C=C2)=NC(=NC1OCCO)C=3N=CC=CN3)C4=C(OC)C=CC=C4.O

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.7555 mL	8.7776 mL	17.5553 mL
5 mM	0.3511 mL	1.7555 mL	3.5111 mL
10 mM	0.1756 mL	0.8778 mL	1.7555 mL
50 mM	0.0351 mL	0.1756 mL	0.3511 mL

Description

Bosentan (Ro 47-0203) is an endothelin (ET) receptor antagonist for and ET-B with 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 [ 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.

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. 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.

References

[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.

Synonyms

Benzenesulfonamide, 4-(1,1-dimethylethyl)-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)[2,2′-bipyrimidin]-4-yl]-, hydrate (1:1)

Benzenesulfonamide, 4-(1,1-dimethylethyl)-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)[2,2′-bipyrimidin]-4-yl]-, monohydrate

Bosentan hydrate

Bosentan monohydrate

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