| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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Arotinolol (Almarl) is a medication acting as a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. It is an antihypertensive medication used to treat both non-cardiovascular and cardiovascular pathologies.
| Targets |
5-HT2A Receptor
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|---|---|
| ln Vitro |
Arotinolol demonstrates the selectivity of β-adrenergic receptors as demonstrated by its binding to rat cerebral cortical membranes with pKi values of 9.74 and 9.26 for β1 and β2 adrenoceptors, respectively, in response to 125I-ICYP. There is equal selectivity between β1 and β2[2].
Arotinolol displaces 125I-ICYP binding to 5HT1B-receptors with the pKi values of 7.97 and 8.16, respectively, for β1 and β2 adrenergic receptors, demonstrating its potency for inhibiting the binding of the same radioligand to the 5HT1B-serotonergic receptor site[2]. |
| ln Vivo |
Arotinolol (oral gavage; 200 mg/kg; 8 weeks) can dramatically lower PWV and CAP. It can also lessen aortic collagen depositions and enhance arterial stiffness in SHR mice[1].
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| Animal Protocol |
SHR mice
200 mg/kg Orally gavage; 200 mg/kg; once daily; 8 weeks |
| References |
| Molecular Formula |
C15H21N3O2S3
|
|---|---|
| Molecular Weight |
371.54114
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| Exact Mass |
371.08
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| Elemental Analysis |
C, 48.49; H, 5.70; N, 11.31; O, 8.61; S, 25.89
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| CAS # |
68377-92-4
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| Related CAS # |
87055-50-3 (R-isomer HCl); 68377-92-4; 92075-58-6 (R-isomer); 68377-91-3 (HCl); 101540-26-5 (S-isomer HCl)
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| Appearance |
Solid powder
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| SMILES |
CC(C)(C)NCC(CSC1=NC(=CS1)C2=CC=C(S2)C(=O)N)O
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| InChi Key |
BHIAIPWSVYSKJS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H21N3O2S3/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)
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| Chemical Name |
5-[2-[3-(tert-butylamino)-2-hydroxypropyl]sulfanyl-1,3-thiazol-4-yl]thiophene-2-carboxamide
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| Synonyms |
Arotinolol; 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) |
DMSO: ~125 mg/mL (~336.4 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.60 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 (5.60 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 (5.60 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 | 2.6915 mL | 13.4575 mL | 26.9150 mL | |
| 5 mM | 0.5383 mL | 2.6915 mL | 5.3830 mL | |
| 10 mM | 0.2692 mL | 1.3458 mL | 2.6915 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01351636 | Completed | Drug: Arotinolol Hydrochloride Drug: Non arotinolol group |
Chronic Kidney Disease | Sumitomo Pharma (Suzhou) Co., Ltd. |
April 2011 | Phase 4 |
| NCT02612298 | Completed | Drug: Arotinolol Hydrochloride Drug: Metoprolol succinate sustained-release tablet |
Essential Hypertension | Sumitomo Pharma (Suzhou) Co., Ltd. |
August 2015 | Phase 4 |
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