| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg | |||
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Oxprenolol HCl (Ba-39089 hydrochloride) is a novel and potent beta blocker with intrinsic sympathomimetic activity. It can be used for the treatment of angina pectoris, abnormal heart rhythms, and high blood pressure. It can be used to treat high blood pressure, irregular cardiac rhythms, and angina pectoris. It inhibits β-adrenergic receptor (β-AR) with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle.
| Targets |
β-adrenoceptor ( Ki = 7.1 nM )
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|---|---|
| ln Vitro |
Oxprenolol is lipophilic [3]. Oxprenolol typically penetrates human abdominal skin at a rate of 1.54 ± 1.54×10-3 cm/h[3].
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| ln Vivo |
Oxprenolol (200 mg/kg/day; oral; once daily for 3 weeks) produces an effective beta-blocker[2].
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| Enzyme Assay |
Binding characteristics of the beta-blockers and beta-agonists with the beta-adrenoceptors were investigated in 3H-dihydroalprenolol (3H-DHA) binding to rat heart membranes treated with neuraminidase. When 60% of the total sialic acid content in the membranes was removed, reproducibility of the binding assay became much better than was attainable without neuraminidase treatment, and the maximum density of beta-adrenoceptors was increased. These data suggest that the binding of the test compounds with the beta-adrenergic receptors in cardiac muscle was under the influence of the sialic acid of the glycocalyx of the membrane. The 3H-DHA binding sites in membranes treated with neuraminidase showed a strict stereo-specificity when tested with propranolol. The ranking order of inhibition of beta-antagonists or agonists is: dl-propranolol > Oxprenolol > than alprenolol > pindolol > YM-09538 > labetalol > acebutolol > atenolol > metoprolol > sotalol > butoxamine > practolol as antagonists or l-isoproterenol > l-epinephrine > l-norepinephrine as agonists. A good correlation (r = 0.91, P less than 0.001) was observed between the Ki values observed by the present binding assay and the pA2 observed in the guinea-pig atria relative to the positive inotropic effect by Bieth et al. (Br. J. Pharmacol. 68, 563-569, 1980), indicating that the present method will be useful for screening new beta-adrenergic receptor antagonists or agonists. [1]
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| Animal Protocol |
Male rats (230 to 300 g body wt) of the Wistar strain
200 mg/kg Administered orally; daily for 3 weeks |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Oral bioavailability is 20-70%. Metabolism/Metabolites Hepatic metabolism. Known human metabolites of oxyprolol include oxyprolol glucuronide. Biological Half-Life 1-2 hours |
| Toxicity/Toxicokinetics |
71172 Female LDLo Oral 90 mg/kg Behavior: General anesthesia; Cardiac: Arrhythmia (including conduction changes); Lung, pleural or respiratory: Cyanosis British Medical Journal, 1(552), 1977
71172 Rat LD50 Oral 214 mg/kg Arzneimittel-Forschung. Drug Research., 35(1236), 1985 [PMID:2866775] 71172 Rat LD50 Intraperitoneal 147 mg/kg Behavior: Somnolence (overall activity inhibition) Kiso to Rinsho. Clinical Reports, 7(3131), 1973 71172 Rat Subcutaneous LD50 940 mg/kg Behavior: Seizures or impact on epileptic threshold; Behavior: Ataxia; Lung, pleural or respiratory: Dyspnea Arzneimittel-Forschung. Drug Research., 18(164), 1968 [PMID:5695373] 71172 Rat intravenous LD50 33 mg/kg Behavioral: seizures or impact on epileptic threshold; Behavioral: ataxia; Lung, pleural or respiratory: dyspnea Arzneimittel-Forschung. Drug Research, 18(164), 1968 [PMID:5695373] |
| References |
|
| Additional Infomation |
Oxyprolol hydrochloride is the hydrochloride salt form of oxyprolol, a lipophilic, non-selective β-adrenergic receptor antagonist with antiarrhythmic, antianginal, and antihypertensive effects. Oxyprolol competitively binds to and blocks the action of β1-adrenergic receptors in the heart, thereby reducing myocardial contractility and heart rate. This leads to a decrease in cardiac output and a reduction in blood pressure. Furthermore, oxyprolol inhibits the release of renin, a hormone secreted by the kidneys that causes vasoconstriction. It is a β-adrenergic antagonist used to treat hypertension, angina pectoris, arrhythmias, and anxiety.
In this study, as a continuation of a previous study (which reported on two β-blockers, celilol and bisoprolol (Modamio et al., 1998)), we compared the in vitro transdermal permeation properties of propranolol, oxpropranolol, metoprolol, and atenolol (including celilol and bisoprolol) through human skin and assessed the potential efficacy of each drug. In addition, we established correlations among the physicochemical parameters of the selected β-blockers, particularly lipophilicity expressed as an intrinsic partition coefficient, to determine whether optimal permeability could be established, thereby assessing the predictive potential of these physicochemical parameters. [3] |
| Molecular Formula |
C15H24CLNO3
|
|---|---|
| Molecular Weight |
301.81
|
| Exact Mass |
301.144
|
| Elemental Analysis |
C, 59.69; H, 8.02; Cl, 11.75; N, 4.64; O, 15.90
|
| CAS # |
6452-73-9
|
| Related CAS # |
Oxprenolol-d7 hydrochloride; 1189649-47-5; Oxprenolol; 6452-71-7; Oxprenolol-d7; 1189805-10-4
|
| PubChem CID |
71172
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| Appearance |
White to off-white solid powder
|
| Boiling Point |
403.3ºC at 760 mmHg
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| Melting Point |
178°C
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| Flash Point |
197.7ºC
|
| LogP |
3.182
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
20
|
| Complexity |
246
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
OC(CNC(C)C)COC1=CC=CC=C1OCC=C.[H]Cl
|
| InChi Key |
COAJXCLTPGGDAJ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C15H23NO3.ClH/c1-4-9-18-14-7-5-6-8-15(14)19-11-13(17)10-16-12(2)3;/h4-8,12-13,16-17H,1,9-11H2,2-3H3;1H
|
| Chemical Name |
1-(propan-2-ylamino)-3-(2-prop-2-enoxyphenoxy)propan-2-ol;hydrochloride
|
| Synonyms |
Dialicor; Coretal; Oxprenolol hydrochloride; 6452-73-9; Oxprenolol HCl; Evinrozit; Ranidrox; Rixiprol; Trasicor; Secondafil; Oxprenolol hydrochloride
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: ~250 mg/mL (~828.3 mM)
H2O: ~100 mg/mL (~331.3 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.89 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 20.8 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: ≥ 2.08 mg/mL (6.89 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 20.8 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: ≥ 2.08 mg/mL (6.89 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 | 3.3133 mL | 16.5667 mL | 33.1334 mL | |
| 5 mM | 0.6627 mL | 3.3133 mL | 6.6267 mL | |
| 10 mM | 0.3313 mL | 1.6567 mL | 3.3133 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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