| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
alpha-adrenergic receptor (antagonist, pA2=6.09); beta-adrenergic receptor (antagonist, pA2=7.73)
|
|---|---|
| ln Vitro |
In the isolated rabbit aortic strip, metroxalol (0.1–10 μM; 20 min) has antagonistic effects on α- and β-adrenergic receptors[1].
In isolated rabbit aortic strips, Medroxalol (0.1-10 microM; 20 min incubation) exhibits antagonistic effects on both alpha- and beta-adrenergic receptors. Cell viability assays demonstrate pA2 values of 6.09 for alpha-adrenergic receptors and 7.73 for beta-adrenergic receptors, indicating its efficacy in blocking these receptor types. |
| ln Vivo |
In spontaneously hypertensive rats, medroxalol (oral gavage; 12.5–50 mg/kg; once daily; 12 d) therapy exhibits antihypertensive activity[1].
Medroxalol shows antihypertensive activity in spontaneously hypertensive rats (SHR). Treatment via oral gavage at doses of 12.5, 25, or 50 mg/kg once daily for 12 days produces a dose-related fall in blood pressure. The vasodilatory effects contribute to its blood pressure-lowering efficacy. |
| Enzyme Assay |
Receptor binding assays for alpha- and beta-adrenergic receptors are performed using membrane preparations from rabbit aortic strips or rat brain cortex. For alpha-adrenergic receptor antagonism, phenylephrine-induced contraction is measured in isolated tissue baths. For beta-adrenergic antagonism, isoproterenol-induced relaxation or chronotropic effects are assessed. pA2 values are calculated from Schild plot analysis.
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: Isolated rabbit aortic strip Tested Concentrations: 0.1-10 μM Incubation Duration: 20 min Experimental Results: demonstrated pA2 values of 6.09 and 7.73 for α-adrenergic receptors and β-adrenergic receptors, respevtively. Cell-based functional assays for adrenergic receptor antagonism use isolated rabbit aortic strips in tissue bath systems. Tissues are pre-contracted with phenylephrine (for alpha) or pre-treated with isoproterenol (for beta). Medroxalol is added at concentrations of 0.1-10 microM and incubated for 20 minutes. Contractile or relaxation responses are measured and expressed as percentage of control. pA2 values are calculated from concentration-response curves. |
| Animal Protocol |
Animal/Disease Models: Male spontaneously hypertensive rats (SHR)[1]
Doses: 12.5, 25, or 50 mg/kg Route of Administration: Oral gavage; 12.5, 25, or 50 mg/kg; one time/day; 12 days Experimental Results: Produced a dose-related fall in blood pressure. In vivo efficacy is evaluated in male spontaneously hypertensive rats (SHR). Medroxalol is administered orally via gavage at 12.5, 25, or 50 mg/kg once daily for 12 days. Blood pressure is measured using tail-cuff plethysmography or telemetry at multiple time points after dosing. Dose-dependent antihypertensive activity is determined by comparing treated groups to vehicle controls. |
| ADME/Pharmacokinetics |
Medroxalol is orally absorbed with good bioavailability. In spontaneously hypertensive rats, it demonstrates dose-dependent antihypertensive activity with sustained effects over the 12-day treatment period. Pharmacokinetic parameters have not been fully characterized but the compound shows sufficient oral exposure to produce vasodilatory and blood pressure-lowering effects at doses of 12.5-50 mg/kg.
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| Toxicity/Toxicokinetics |
Toxicology data for Medroxalol are limited as it is a research compound. Standard preclinical safety assessment would include acute toxicity studies in rodents and repeat-dose toxicity studies (14-90 days) in rats and dogs to identify target organ toxicity. As an alpha/beta antagonist, potential side effects include bradycardia, hypotension, and bronchospasm.
|
| References |
[1]. Dage RC, et al. Cardiovascular properties of medroxalol, a new antihypertensive drug. J Cardiovasc Pharmacol. 1981 Mar-Apr;3(2):299-315.
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| Additional Infomation |
Medroxalol belongs to the salicylamide class of drugs.
Medroxalol is an investigational adrenergic receptor antagonist that blocks both alpha- and beta-adrenergic receptors with pA2 values of 6.09 (alpha) and 7.73 (beta). Its dual blocking mechanism produces antihypertensive and vasodilatory effects. As of current information, Medroxalol has not received regulatory approval for clinical use and remains in the research stage for cardiovascular indications. |
| Molecular Formula |
C20H24N2O5
|
|---|---|
| Molecular Weight |
372.41
|
| Exact Mass |
372.169
|
| CAS # |
56290-94-9
|
| Related CAS # |
70161-10-3 (mono-hydrochloride)
|
| PubChem CID |
41835
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.307g/cm3
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| Boiling Point |
604.1ºC at 760 mmHg
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| Flash Point |
319.1ºC
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| Index of Refraction |
1.626
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| LogP |
2.955
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| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
8
|
| Heavy Atom Count |
27
|
| Complexity |
491
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC(CCC1=CC2=C(C=C1)OCO2)NCC(C3=CC(=C(C=C3)O)C(=O)N)O
|
| InChi Key |
MPQWSYJGFLADEW-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H24N2O5/c1-12(2-3-13-4-7-18-19(8-13)27-11-26-18)22-10-17(24)14-5-6-16(23)15(9-14)20(21)25/h4-9,12,17,22-24H,2-3,10-11H2,1H3,(H2,21,25)
|
| Chemical Name |
5-[2-[4-(1,3-benzodioxol-5-yl)butan-2-ylamino]-1-hydroxyethyl]-2-hydroxybenzamide
|
| 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)
|
| Solubility (In Vitro) |
DMSO: 50 mg/mL (134.26 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6852 mL | 13.4261 mL | 26.8521 mL | |
| 5 mM | 0.5370 mL | 2.6852 mL | 5.3704 mL | |
| 10 mM | 0.2685 mL | 1.3426 mL | 2.6852 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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