| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
In the presence of 30 μM propranolol, isoproterenol-induced relaxation is modified by buprolol (1~3 μM). Buprolol has a pA2 value of 5.90 and functions as a competitive antagonist of isoproterenol-induced relaxation in the presence of 300 nM propranolol. With a pA2 value of roughly 9.0, buprolol antagonizes β1- and β2-AR. It also antagonizes β3-AR, with a pA2 value of 6.0 [1].
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Quickly and completely absorbed from the gut with less than 10% oral bioavailability. Metabolism / Metabolites Over 90% undergoes first-pass metabolism. The main metabolite is carboxybupranolol, 4-chloro-3-[3-(1,1-dimethylethylamino)-2-hydroxy-propyloxy]benzoic acid, of which 88% are eliminated renally within 24 hours. Biological Half-Life 2-4 hours |
| Toxicity/Toxicokinetics |
Protein Binding
76% |
| References |
[1]. Chino D, et al. Pharmacological identification of β-adrenoceptor subtypes mediating isoprenaline-induced relaxation of guinea pig colonic longitudinal smooth muscle. J Smooth Muscle Res. 2018;54(0):13-27.
[2]. Babu RJ, et al. Effect of cyclodextrins on the complexation and transdermal delivery of bupranolol through rat skin. Int J Pharm. 2004;271(1-2):155-165. |
| Additional Infomation |
Bupranolol is an aromatic ether.
Bupranolol is a non-selective beta blocker with potency similar to [propanolol]. It does not have intrinsic sympathomimetic activity (ISA), but does have strong membrane stabilizing activity. An adrenergic-beta-2 antagonist that has been used for cardiac arrhythmia, angina pectoris, hypertension, glaucoma, and as an antithrombotic. Drug Indication Used to manage hypertension and tachycardia. Also used to treat glaucoma. Mechanism of Action Bupranolol competes with sympathomimetic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart, inhibiting sympathetic stimulation. This results in a reduction in resting heart rate, cardiac output, systolic and diastolic blood pressure, and reflex orthostatic hypotension. Pharmacodynamics Bupranolol is a competitive, nonselective beta-blocker similar to propanolol without intrinsic sympathomimetic activity. |
| Molecular Formula |
C14H22NO2CL
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|---|---|
| Molecular Weight |
271.78298
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| Exact Mass |
271.134
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| CAS # |
14556-46-8
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| PubChem CID |
2475
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.098g/cm3
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| Boiling Point |
396.3ºC at 760mmHg
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| Flash Point |
193.5ºC
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| Vapour Pressure |
5.44E-07mmHg at 25°C
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| Index of Refraction |
1.522
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| LogP |
3.167
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
18
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| Complexity |
242
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C=CC(C)=CC=1OCC(O)CNC(C)(C)C
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| InChi Key |
HQIRNZOQPUAHHV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H22ClNO2/c1-10-5-6-12(15)13(7-10)18-9-11(17)8-16-14(2,3)4/h5-7,11,16-17H,8-9H2,1-4H3
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| Chemical Name |
1-(tert-butylamino)-3-(2-chloro-5-methylphenoxy)propan-2-ol
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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 |
| 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) |
DMSO : ~50 mg/mL (~183.97 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.20 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 (9.20 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 (9.20 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6794 mL | 18.3972 mL | 36.7945 mL | |
| 5 mM | 0.7359 mL | 3.6794 mL | 7.3589 mL | |
| 10 mM | 0.3679 mL | 1.8397 mL | 3.6794 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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