Size | Price | Stock | Qty |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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Purity: ≥98%
Bosentan (formerly Ro 47-0203; brand name Tracleer) is a potent, competitive and dual antagonist of endothelin (ET) receptor with anti-hypertensive activity. It inhibits ET-A and ET-B with Ki values of 4.7 nM and 95 nM, respectively. Bosentan is used to treat pulmonary arterial hypertension (PAH) as a vasodilator.
Targets |
ETA receptor ( Ki = 4.7 nM ); ETA receptor ( Ki = 95 nM )
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ln Vitro |
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ln Vivo |
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Cell Assay |
The trypan blue exclusion test is used to assess the viability of cells. Bosentan is added to human dermal fibroblasts at the recommended concentrations (10, 20 and 40 μM). After 24 and 48 hours, cell viability is assessed. A hematocytometer is used to count both stained (dead) and unstained (viable) cells[2].
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Animal Protocol |
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References |
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Molecular Formula |
C27H29N5O6S
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Molecular Weight |
551.61
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Exact Mass |
551.18
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Elemental Analysis |
C, 58.79; H, 5.30; N, 12.70; O, 17.40; S, 5.81
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CAS # |
147536-97-8
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Appearance |
Solid powder
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SMILES |
CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)NC2=C(C(=NC(=N2)C3=NC=CC=N3)OCCO)OC4=CC=CC=C4OC
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InChi Key |
GJPICJJJRGTNOD-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C27H29N5O6S/c1-27(2,3)18-10-12-19(13-11-18)39(34,35)32-23-22(38-21-9-6-5-8-20(21)36-4)26(37-17-16-33)31-25(30-23)24-28-14-7-15-29-24/h5-15,33H,16-17H2,1-4H3,(H,30,31,32)
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Chemical Name |
4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-pyrimidin-2-ylpyrimidin-4-yl]benzenesulfonamide
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.8129 mL | 9.0644 mL | 18.1288 mL | |
5 mM | 0.3626 mL | 1.8129 mL | 3.6258 mL | |
10 mM | 0.1813 mL | 0.9064 mL | 1.8129 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT02116335 | Active Recruiting |
Drug: Bosentan Drug: Placebo |
Hypertension | Augusta University | June 2015 | Not Applicable |
NCT05657613 | Active Recruiting |
Drug: Part 2 -Group A Bosentan 125 mg (CYP450 3A4 inducer) with Pacritinib |
Drug Interactions | CTI BioPharma | January 3, 2023 | Phase 1 |
NCT02377271 | Recruiting | Drug: bosentan Drug: placebo |
Ischemic Optic Neuropathy | University Hospital, Grenoble | August 2015 | Phase 3 |
NCT04158635 | Recruiting | Drug: Bosentan Drug: Gemcitabine Drug: Nab-paclitaxel |
Stage III Pancreatic Cancer AJCC v8 Stage IV Pancreatic Cancer AJCC v8 |
City of Hope Medical Center | September 1, 2021 | Phase 1 |
NCT04039464 | Recruiting | Drug: Duo-Therapy with Sildenafil + Bosentan |
Pediatric Pulmonary Hypertension |
Johns Hopkins University | August 1, 2022 | Phase 3 |
Bosentan reversed the pro-fibrotic phenotype of systemic sclerosis (SSc) dermal fibroblasts via increasing the DNA binding of Fli1. Arthritis Res Ther . 2014 Apr 3;16(2):R86. td> |
Bosentan prevented the development of dermal fibrosis, at least partially, by increasing the expression of Fli1 protein in lesional dermal fibroblasts of bleomycin (BLM)-induced systemic sclerosis (SSc) murine model. Arthritis Res Ther . 2014 Apr 3;16(2):R86. td> |
Absence of pharmacological activity of bosentan on top of macitentan in conscious Dahl-salt sensitive rats. Life Sci . 2014 Nov 24;118(2):333-9. td> |
Superior pharmacological effect of macitentan on top of bosentan in conscious bleomycin-induced pulmonary hypertensive rats. Life Sci . 2014 Nov 24;118(2):333-9. td> |
Experimental design and time schedule. Ligature was placed on day 0, and bosentan was treated 1 day before ligature ligation (-1 day). PLoS One . 2016 Dec 28;11(12):e0167713. td> |