Bosentan Hydrate

Catalog No.S3051 Batch:S305102

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Technical Data

Formula

C27H29N5O6S.H2O
Molecular Weight 569.63 CAS No. 157212-55-0
Solubility (25°C)* In vitro DMSO 100 mg/mL (175.55 mM)
Ethanol 60 mg/mL (105.33 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% Corn oil
0.65mg/ml Taking the 1 mL working solution as an example, add 50 μL of 13 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Bosentan (Ro 47-0203) 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]
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]

Protocol (from reference)

Animal Study:[1]
  • Animal Models

    Male Wistar rats with CHF

  • Dosages

    100 mg/kg, 30 mg/kg

  • Administration

    Oral

Selleck's Bosentan Hydrate has been cited by 11 publications

Metformin and simvastatin synergistically suppress endothelin 1-induced hypoxia and angiogenesis in multiple cancer types [ Cancer Sci, 2023, 114(2):640-653] PubMed: 36156330
Fibrocytes boost tumor-supportive phenotypic switches in the lung cancer niche via the endothelin system [ Nat Commun, 2022, 13(1):6078] PubMed: 36241617
Additive protective effects of sacubitril/valsartan and bosentan on vascular remodelling in experimental pulmonary hypertension [ Cardiovasc Res, 2021, 117(5):1391-1401] PubMed: 32653925
Endothelin-1 as a Mediator of Heme Oxygenase-1-Induced Stemness in Colorectal Cancer: Influence of p53 [ J Pers Med, 2021, 11(6)509] PubMed: 34199777
Endothelin Inhibition Potentiates Cancer Immunotherapy Revealing Mechanical Biomarkers Predictive of Response [ Wiley Online Library, 2021, 10.1002/adtp.202000289] PubMed: None
Effect of Puerarin on Action Potential and Sodium Channel Activation in Human Hypertrophic Cardiomyocytes [ Biosci Rep, 2020, 28;40(2):BSR20193369] PubMed: 32003781
HDAC inhibition enhances the in vivo efficacy of MEK inhibitor therapy in uveal melanoma [ Clin Cancer Res, 2019, 10.1158/1078-0432] PubMed: 31227503
S-nitrosation impairs KLF4 activity and instigates endothelial dysfunction in pulmonary arterial hypertension. [ Redox Biol, 2019, 21:101099] PubMed: 30660098
Role of endothelin-1 clearance in the haemodynamic responses to endothelin-1 in the pulmonary and hindquarter vasculature of anaesthetised rats. [ Eur J Pharmacol, 2019, 855:124-136] PubMed: 31063771
Notch signaling activation induces cell death in MAPKi-resistant melanoma cells [ Pigment Cell Melanoma Res, 2019, 32(4):528-539] PubMed: 30614626

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.