Bosentan Hydrate

製品コードS3051 バッチS305102

印刷

化学情報

Chemical Structure Synonyms Ro 47-0203 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C27H29N5O6S.H2O
分子量 569.63 CAS No. 157212-55-0
Solubility (25°C)* 体外 DMSO 100 mg/mL (175.55 mM)
Ethanol 60 mg/mL (105.33 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
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. 
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. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
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]

プロトコル(参考用のみ)

キナーゼアッセイ 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.
動物実験 動物モデル Male Wistar rats with CHF
投薬量 100 mg/kg, 30 mg/kg
投与方法 Oral

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。