(S)-(-)-Atenolol |
رقم الكتالوجGC12463 |
(S)-(-)-Atenolol is a potent β-adrenergic receptor blocker. (S)-(-)-Atenolol is the S(-) enantiomer of Atenolol, while the R(+) enantiomer of Atenolol has almost no β-receptor blocker activity.
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Cas No.: 93379-54-5
Sample solution is provided at 25 µL, 10mM.
(S)-(-)-Atenolol is a potent β-adrenergic receptor blocker[1]. (S)-(-)-Atenolol is the S(-) enantiomer of Atenolol, while the R(+) enantiomer of Atenolol has almost no β-receptor blocker activity[2, 3]. (S)-(-)-Atenolol is mainly used to treat hypertension and heart-related chest pain[4].
In vitro, (S)-(-)-Atenolol (0-350μM) treated vascular smooth muscle A7r5 cells for 24h inhibited cell viability in a dose-dependent manner and reduced the levels of calmodulin and annexin A6 in the cells[5]. (S)-(-)-Atenolol (200, 400, 600μM) treated MCF7 cells for 72h significantly inhibited cell migration and reduced the percentage of wound healing (WH) of the cells[6].
In vivo, (S)-(-)-Atenolol (90mg/kg/day) was orally administered to spontaneously hypertensive rats for 8 weeks and was less effective in reducing carotid systolic blood pressure than Carvedilol (30mg/kg/day) or Nebivolol (30mg/kg/day)[7].
References:
[1] Mehvar R, Brocks D R. Stereospecific pharmacokinetics and pharmacodynamics of beta-adrenergic blockers in humans[J]. 2001.
[2] Seebauer C T, Graus M S, Huang L, et al. Non–beta blocker enantiomers of propranolol and atenolol inhibit vasculogenesis in infantile hemangioma[J]. The Journal of Clinical Investigation, 2022, 132(3).
[3] Stoschitzky K, Egginger G, Zernig G, et al. Stereoselective features of (R)‐and (S)‐atenolol: Clinical pharmacological, pharmacokinetic, and radioligand binding studies[J]. Chirality, 1993, 5(1): 15-19.
[4] Heel R C, Brogden R N, Speight T M, et al. Atenolol: a review of its pharmacological properties and therapeutic efficacy in angina pectoris and hypertension[J]. Drugs, 1979, 17: 425-460.
[5] Sui J, Zhang J, Tan T L, et al. Comparative proteomics analysis of vascular smooth muscle cells incubated with S-and R-enantiomers of atenolol using iTRAQ-coupled two-dimensional LC-MS/MS[J]. Molecular & Cellular Proteomics, 2008, 7(6): 1007-1018.
[6] İşeri Ö D, Sahin F I, Terzi Y K, et al. beta-Adrenoreceptor antagonists reduce cancer cell proliferation, invasion, and migration[J]. Pharmaceutical biology, 2014, 52(11): 1374-1381.
[7] Del Mauro J S, Prince P D, Allo M A, et al. Effects of third-generation β-blockers, atenolol or amlodipine on blood pressure variability and target organ damage in spontaneously hypertensive rats[J]. Journal of Hypertension, 2020, 38(3): 536-545.
Cell experiment [1]: | |
Cell lines | A7r5 cells |
Preparation Method | After reaching 80% confluence the cells were incubated with 0-350μM (R)-(+)-Atenolol and (S)-(-)-Atenolol for 24h, in the absence of serum. The viability was examined by the MTT assay. |
Reaction Conditions | 0-350μM; 24h |
Applications | The two enantiomers of Atenolol was toxic to the cells with a drastic decrease in cell viability for any concentration higher than 50μM. The (R)-(+)-Atenolol was somewhat less toxic than the (S)-(-)-Atenolol. |
Animal experiment [2]: | |
Animal models | Spontaneously hypertensive rats (SHR) |
Preparation Method | SHR rats received Carvedilol 30mg/kg, Nebivolol 30mg/kg, (S)-(-)-Atenolol 90mg/kg, Amlodipine 10mg/kg or vehicle by oral gavage once a day for 8 weeks. WKY rats administered with vehicle were used as normotensive control group. |
Dosage form | 90mg/kg/day for 8 weeks; p.o. |
Applications | Chronic treatment with Carvedilol or Nebivolol attenuates carotid BP and short-term BPV, and reduces target organ damage in SHR to a greater extent than (S)-(-)-Atenolol. |
References: |
Cas No. | 93379-54-5 | SDF | |
Chemical Name | (S)-2-(4-(2-hydroxy-3-(isopropylamino)propoxy)phenyl)acetamide | ||
Canonical SMILES | O[C@H](COC1=CC=C(CC(N)=O)C=C1)CNC(C)C | ||
Formula | C14H22N2O3 | M.Wt | 266.34 |
الذوبان | Soluble to 25 mM in sterile water | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
1 mM | 3.7546 mL | 18.773 mL | 37.546 mL |
5 mM | 0.7509 mL | 3.7546 mL | 7.5092 mL |
10 mM | 0.3755 mL | 1.8773 mL | 3.7546 mL |
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- Purity: >99.50%
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