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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5g |
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Other Sizes |
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Purity: ≥98%
Bosentan Hydrate (also known as Ro 47-0203; Ro47-0203; Ro-47-0203; Tracleer) is a potent, competitive and dual endothelin (ET) A/B receptor antagonist for ET-A and ET-B with anti-hypertensive activity. It inhibits ET-A and ET-B with Ki values of 4.7 nM and 95 nM, respectively. Bosentan is an authorized drug used as a vasodilator to treat pulmonary arterial hypertension. Bosentan is an ETBR and ETAR inhibitor. It is applied to the management of PAH, or pulmonary arterial hypertension. Bosentan prevents endothelin molecules from acting, which would otherwise encourage blood vessel narrowing and raise blood pressure.
Targets |
ET-A ( Ki = 4.7 nM ); ET-B ( 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 determine the viability of cells. Bosentan is applied to human dermal fibroblasts at the recommended concentrations (10, 20 and 40 μM). Viability of the cells is assessed after 24 and 48 hours. Using a hematocytometer, the number of stained (dead) and unstained (viable) cells is determined.
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Animal Protocol |
Rats: Rats that are two months old—DSS and Wistar—are employed. Doses ranging from 0.1 to 100 mg/kg (Macitentan) or 3 to 600 mg/kg (Bosentan) are used to measure the pharmacological effects on heart rate (HR), mean arterial pressure (MAP), or mean pulmonary arterial pressure (MPAP), and up to 120 hours after a single gavage. 1) Macitentan is given on top of the maximum effective dose of Bosentan determined by the dose-response curve in order to assess whether Macitentan can offer greater pharmacological activity compared to Bosentan. Secondly, the maximum effective dose of Macitentan is topped off with the same dose of Bosentan. Tmax of the first tested compound is the point at which the second compound's maximal effective dose is given.
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References |
Molecular Formula |
C27H31N5O7S
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Molecular Weight |
569.63
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Exact Mass |
569.19
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CAS # |
157212-55-0
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Appearance |
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.O
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InChi Key |
SXTRWVVIEPWAKM-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C27H29N5O6S.H2O/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);1H2
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Chemical Name |
4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-pyrimidin-2-ylpyrimidin-4-yl]benzenesulfonamide;hydrate
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Synonyms |
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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 | 1.7555 mL | 8.7776 mL | 17.5553 mL | |
5 mM | 0.3511 mL | 1.7555 mL | 3.5111 mL | |
10 mM | 0.1756 mL | 0.8778 mL | 1.7555 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.