| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
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| Other Sizes |
Purity: ≥98%
| Targets |
Arotinolol hydrochloride targets both α- and β-adrenergic receptors. It shows high affinities for both β1- and β2-adrenoceptors and a moderate affinity for α-adrenoceptors. It also shows the ability to inhibit radioligand binding to 5-HT1B serotonin receptors. By blocking α- and β-adrenergic receptors, arotinolol reduces heart rate, cardiac output, and peripheral vascular resistance.
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| ln Vitro |
In vitro, arotinolol hydrochloride shows high affinities for both β1- and β2-adrenoceptors. It also shows a moderate affinity for α-adrenoceptors. It inhibits radioligand binding to 5-HT1B serotonin receptors. These in vitro activities confirm its profile as a nonselective α/β-adrenergic receptor blocker with additional serotonergic receptor affinity.
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| ln Vivo |
In vivo, arotinolol hydrochloride is an antihypertensive agent used for the treatment of hypertension, angina pectoris, and arrhythmias. It is widely used in the treatment of high blood pressure. Its clinical efficacy has been established in numerous studies. It is available as a prescription medication for cardiovascular diseases.
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| Enzyme Assay |
The in vitro receptor binding assay for arotinolol hydrochloride typically involves radioligand displacement studies using membrane preparations from cells expressing adrenergic receptors. The compound's affinity for β1-, β2-, and α-adrenoceptors is determined. Its affinity for 5-HT1B serotonin receptors is also assessed. These cell-free assays provide a direct measure of the compound's binding profile.
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| Cell Assay |
In vitro cellular assays for arotinolol hydrochloride assess its functional antagonism at adrenergic receptors. Cells expressing β- or α-adrenergic receptors are stimulated with appropriate agonists, and the compound's ability to inhibit downstream signaling is measured. These assays demonstrate the compound's functional antagonism at its target receptors in a relevant cellular context.
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| Animal Protocol |
In vivo animal studies for arotinolol hydrochloride have been conducted in animal models of hypertension to assess its antihypertensive effects. However, the compound's clinical efficacy has been established in human clinical trials. It is approved for clinical use in hypertension, angina pectoris, and arrhythmias.
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| ADME/Pharmacokinetics |
Arotinolol hydrochloride is administered orally. It is absorbed and distributed throughout the body. It is metabolized in the liver and excreted in urine. Its pharmacokinetic properties support its use as an antihypertensive agent. However, specific parameters such as half-life and bioavailability are not extensively detailed in the available literature.
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| Toxicity/Toxicokinetics |
Arotinolol hydrochloride has a well-established safety profile. Common adverse effects include bradycardia, dizziness, and fatigue. It may cause bronchoconstriction in patients with asthma due to its β2-blocking activity. Its safety has been established through extensive clinical use. It is available as a prescription medication.
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| References |
Wang Z, Zhang X, Jiang S, Guo X. Magnetic solid-phase extraction based on magnetic multiwalled carbon nanotubes for the simultaneous enantiomeric analysis of five β-blockers in the environmental samples by chiral liquid chromatography coupled with tandem mass spectrometry. Talanta. 2018 Apr 1;180:98-107. doi: 10.1016/j.talanta.2017.12.034. Epub 2017 Dec 14. PubMed PMID: 29332839.
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| Additional Infomation |
Alotinol hydrochloride is an aromatic amide, belonging to the thiophene class of compounds.
Arotinolol hydrochloride (Almarl) is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. It shows high affinities for both β1- and β2-adrenoceptors and a moderate affinity for α-adrenoceptors. It is an antihypertensive agent used for the treatment of hypertension, angina pectoris, and arrhythmias. It is available as a prescription medication. |
| Molecular Weight |
408.0021
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|---|---|
| Exact Mass |
407.056
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| CAS # |
68377-91-3
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| Related CAS # |
68377-92-4;68377-91-3 (HCl);87055-50-3 (R-isomer HCl);92075-58-6 (R-isomer); 101540-26-5 (S-isomer HCl);
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| PubChem CID |
155032
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.35g/cm3
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| Boiling Point |
599.8ºC at 760mmHg
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| Melting Point |
234-235.5° (dec)
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| Flash Point |
316.6ºC
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| LogP |
4.704
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
24
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| Complexity |
406
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl[H].S(C1=NC(=C([H])S1)C1=C([H])C([H])=C(C(N([H])[H])=O)S1)C([H])([H])C([H])(C([H])([H])N([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])O[H]
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| InChi Key |
XXDAXBZYUXLDRD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H21N3O2S3.ClH/c1-15(2,3)17-6-9(19)7-21-14-18-10(8-22-14)11-4-5-12(23-11)13(16)20/h4-5,8-9,17,19H,6-7H2,1-3H3,(H2,16,20)1H
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| Chemical Name |
2-Thiophenecarboxamide,
5-(2-((3-((1,1-dimethylethyl)amino)-2-hydroxypropyl)thio)-4-thiazolyl)-,
monohydrochloride, (+-)-
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| Synonyms |
Almarl
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.4510 mL | 12.2549 mL | 24.5098 mL | |
| 5 mM | 0.4902 mL | 2.4510 mL | 4.9020 mL | |
| 10 mM | 0.2451 mL | 1.2255 mL | 2.4510 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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