Bosentan Hydrate

Catalog No.S3051

Bosentan is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively.

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Bosentan Hydrate Chemical Structure

Bosentan Hydrate Chemical Structure
Molecular Weight: 569.63

Validation & Quality Control

Quality Control & MSDS

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Product Information

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Product Description

Biological Activity

Description Bosentan is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively.
Targets ET-A [1] ET-B [1]
IC50 4.7 nM(Ki) 95 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]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

Selectivity Assay The specificity of bosentan as an ET receptor antagonist is assessed by testing any possible interference with the binding of other regulatory agents. The binding of neurotransmitters (adenosine, catecholamines, acetylcholine, γ-amino-n-butyric acid, histamine, serotonin and glutamate), neuropeptides or intestinal peptides or growth factors (platelet-derived growth factor, transforming growth factor-β, angiotensin, arginine-vasopressin, bombesin, bradykinin, cholecystokinin, calcitonin gene-related peptide, substance P, neurokinin A, neuropeptide Y, neurotensin, somatostatin, thyrotropin-releasing hormone, vasoactive intestinal peptide, oxytocin and platelet activating factor), eicosanoids (leukotriene B4 and thromboxane A2) and ions (chloride, potassium and calcium) is tested using radiolabeled ligands and corresponding receptor preparations.

Animal Study: [1]

Animal Models Male Wistar rats with CHF
Formulation 5% gum arabic and prepared freshly every day
Dosages 100 mg/kg, 30 mg/kg
Administration Oral

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

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.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-06-25)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02798055 Not yet recruiting Systematic Sclerosis|Digital Ulcer|Scleroderma Elpen Pharmaceutical Co. Inc. June 2016 --
NCT02667704 Completed Healthy Boehringer Ingelheim February 2016 Phase 1
NCT02480335 Not yet recruiting Scleroderma, Systemic University Medical Center Groningen|Actelion June 2015 Phase 4
NCT02116335 Recruiting Hypertension Georgia Regents University|National Heart, Lung, and Bloo  ...more Georgia Regents University|National Heart, Lung, and Blood Institute (NHLBI) June 2015 --
NCT02377271 Not yet recruiting Ischemic Optic Neuropathy University Hospital, Grenoble March 2015 Phase 3

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Chemical Information

Download Bosentan Hydrate SDF
Molecular Weight (MW) 569.63
Formula

C27H29N5O6S.H2O

CAS No. 157212-55-0
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms Ro 47-0203
Solubility (25°C) * In vitro DMSO 100 mg/mL (175.55 mM)
Ethanol 2 mg/mL (3.51 mM)
Water 0.001 mg/mL (0.0 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Benzenesulfonamide, 4-(1,1-dimethylethyl)-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)[2,2'-bipyrimidin]-4-yl]-, hydrate (1:1)

Tech Support

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