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Bosentan hydrate

Product Name
Bosentan hydrate
CAS No.
157212-55-0
Chemical Name
Bosentan hydrate
Synonyms
CS-170;Bosetan;bosentan hydrate;Bosentan (200 mg);Bosentan (1076115);Bosentan monohydrate;Bosentan hydrate USP/EP/BP;Bosentan Hydrate See B675900;Bosentan Hydrate (Ro 47-0203);Tracleer, Bosentan monohydrate
CBNumber
CB6547457
Molecular Formula
C27H31N5O7S
Formula Weight
569.62934
MOL File
157212-55-0.mol
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Bosentan hydrate Property

Melting point:
114-118 °C
storage temp. 
2-8°C
solubility 
DMSO (Slightly), Methanol (Very Slightly, Heated)
form 
powder
color 
white to beige
Merck 
14,1353
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Safety

HS Code 
2935909550
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML1265
Product name
Bosentan hydrate
Purity
≥98% (HPLC)
Packaging
10MG
Price
$108
Updated
2023/06/20
Sigma-Aldrich
Product number
SML1265
Product name
Bosentan hydrate
Purity
≥98% (HPLC)
Packaging
50MG
Price
$438
Updated
2023/06/20
Sigma-Aldrich
Product number
PHR2708
Product name
Bosentan
Purity
certified reference material, pharmaceutical secondary standard
Packaging
500MG
Price
$349
Updated
2022/05/15
Sigma-Aldrich
Product number
1076115
Product name
Bosentan
Purity
United States Pharmacopeia (USP) Reference Standard
Packaging
200MG
Price
$818
Updated
2022/05/15
TCI Chemical
Product number
B5118
Product name
Bosentan Monohydrate
Purity
>98.0%(HPLC)
Packaging
25mg
Price
$57
Updated
2024/03/01
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Bosentan hydrate Chemical Properties,Usage,Production

Uses

Antagonist (endothelin receptor).

Uses

Bosentan hydrate has been used in cell viability assay. It has also been used as a positive control for calcium transient analysis.

Definition

ChEBI: Bosentan hydrate is a hydrate. It contains a bosentan.

brand name

Tracleer (Actelion).

Biological Activity

a sulfonamide-derived, competitive and specific endothelin receptor antagonist with a relatively higher affinity to the endothelin a receptor than endothelin b receptor. by competitively binding to endothelin a and endothelin b receptors in the endothelium and vascular smooth muscle, bosentan offset the effect of endothelin which is an extremely potent endogenous vasoconstrictor and broncho-constrictor. in addition, bosentan decreases both pulmonary and systemic vascular resistance and is particularly applied in the treatment of pulmonary arterial hypertension. [1]

Biochem/physiol Actions

Bosentan is an endothelin receptor antagonist. Endothelin is a potent vasoconstrictor, making antagonists of clinical interest for the treatment of conditions associated with vasospasm, such as subarachnoid hemorrhage (SAH) and hypertension. Bosentan is a dual endothelin receptor antagonist effective in the treatment of pulmonary arterial hypertension (PAH), the first of the class to make it to market. Bosentan is an orally available, competitive antagonist of both the ETA and ETB receptor subtypes with a Ki of 4.7 nM for ETA and a Ki of 95 nM for ETB.

in vitro

a study was performed in vitro to measure the influence of bosentan on the angiogenic performance of dermal microvascular endothelial cells (mvecs) and to detect the capacity of bosentan in offsetting the antiangiogenic effects of systemic sclerosis sera. it was found that bosentan significantly increased cell viability and offset the antiangiogenic effects of systemic sclerosis sera on dermal mvecs. [2]

in vivo

a study was conducted to investigate the effect of bosentan on plasma leptin level after myocardial infarction in wistar rats. after oral administration of bosentan once daily at the dose of 100 mg/kg for 2 days, concentration of leptin in plasma significantly increased. this finding revealed that bosentan played an crucial role on regulating leptin concentration in ischemic cardiovascular pathology. [1]

IC 50

inhibiting endothelin receptor a and b with an ic50 of 15.1 ± 1.6 μm in p388/dx cells.

References

[1] ostrowski rp, januszewski sa, kowalska za and kapuscinski a. effect of endothelin receptor antagonist bosentan on plasma leptin concentration in acute myocardial infarction in rats. pathophysiology. 2003 sep; 9(4): 249-56.
[2]romano e, bellando-randone s, manetti m, bruni c, lepri g, matucci-cerinic m, guiducci s. bosentan blocks the antiangiogenic effects of sera from systemic sclerosis patients: an in vitro study. clin exp rheumatol. 2015 aug; 33(4 suppl 91): s148-52.
[3]rubin lj, badesch db, barst rj, galiè n, black cm et, al. bosentan therapy for pulmonary arterial hypertension. new engl j med. 2002 mar; 346 (12): 896-903.

Bosentan hydrate Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Bosentan hydrate manufacturers

Wuhan Nutra Biotechnology Co.,Ltd
Product
Bosentan hydrate 157212-55-0
Price
US $0.00-0.00/g
Min. Order
1g
Purity
98%+
Supply Ability
100kgs
Release date
2021-05-24
Qiuxian Baitai New Material Co., LTD
Product
Bosentan hydrate 157212-55-0
Price
US $0.20/g
Min. Order
100g
Purity
99.99%
Supply Ability
5ton/Month
Release date
2021-11-26
Zhuozhou Wenxi import and Export Co., Ltd
Product
Bosentan hydrate 157212-55-0
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-10

157212-55-0, Bosentan hydrateRelated Search:


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  • C27H29N5O6SH2O
  • 9N5O6SH2O
  • C27H31N5O7S
  • C27H29N5O6S2O
  • Inhibitors
  • API
  • Heterocyclic Compounds