| 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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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 | ||
| Additional Infomation |
Bosentan hydrate is a hydrate. It contains a bosentan.
A sulfonamide and pyrimidine derivative that acts as a dual endothelin receptor antagonist used to manage PULMONARY HYPERTENSION and SYSTEMIC SCLEROSIS. See also: Bosentan (annotation moved to). |
| Molecular Formula |
C27H31N5O7S
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| Molecular Weight |
569.63
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| Exact Mass |
569.194
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| CAS # |
157212-55-0
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| Related CAS # |
Bosentan; 147536-97-8
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| PubChem CID |
185462
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| Appearance |
White to off-white solid powder
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| Boiling Point |
742.3ºC at 760 mmHg
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| Flash Point |
402.8ºC
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| Vapour Pressure |
3.84E-23mmHg at 25°C
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| LogP |
5.293
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
40
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| Complexity |
839
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| Defined Atom Stereocenter Count |
0
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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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| 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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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.39 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.39 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.39 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (4.39 mM) (saturation unknown) in 10% EtOH + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: ≥ 2.5 mg/mL (4.39 mM) (saturation unknown) in 10% EtOH + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. |
| 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.
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