Labetalol hydrochloride
Based on 5 publication(s) in Google Scholar
Labetalol (AH5158) hydrochloride is an orally available, selective α1-adrenergic recepto and non-selective β-adrenergic receptor competitive antagonist. Labetalol hydrochloride is an antihypertensive molecule that partially crosses the blood-brain barrier and has little effect on cardiac output. Labetalol hydrochloride can be used in the study of cardiovascular diseases, such as hypertension during pregnancy.
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- Purity: 99.90%
- CAS No.: 32780-64-6
- 화학식: C19H25ClN2O3
- 분자량:364.87
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보관:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Labetalol hydrochloride (Standard)
Publications Citing Use of MedChemExpress (MCE) Labetalol hydrochloride
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In Vivo Efficacy Study
All Adrenergic Receptor Isoforms
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Biological Activity
Labetalol hydrochloride exhibits greater affinity for the β-adrenergic sites on guinea pig cardiac and lung membranes (IC50=0.8 and 4.0 μM, respectively)[1].
Labetalol hydrochloride has an affinity for the α-adrenergic binding site on rabbit uterine membranes (IC50=15 μM). Labctalol has a 19-fold greater binding affinity for the β-binding site in cardiac membranes than for the α-binding site in uterine membranes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Labetalol (10 mg/kg; subcutaneous injection; twice daily; 10 days) hydrochloride significantly increases hypothalamic α1 receptor binding and elevates the ratio of norepinephrine metabolites MHPG/NA in neonatal Wistar rats, but does not cause long-term changes in receptor density in adulthood[2].
Labetalol (10 mg/kg; ih) crosses the blood-brain barrier and reaches 2.1 μg/g tissue level in the brain of 10-day-old rats 90 minutes after injection[2].
Labetalol (5.0 mg/kg; ip) hydrochloride attenuates circulating IL-1β and IL-6 in tail-shock stressed rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult mongrel dogs (gender not specified, weight 225-300 g)[2]
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Dosage:0.63 mg/kg, 6.3 mg/kg (saline)
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Administration:Intravenous injection, single dose
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Result:Low-dose Labetalol (0.63 mg/kg) preferentially blocked β-adrenergic responses, while high-dose (6.3 mg/kg) significantly blocked α-adrenergic responses in anesthetized dogs.
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Animal Model:Male Wistar rats (postnatal day 1-10)[3]
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Dosage:10 mg/kg (saline)
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Administration:Subcutaneous injection, twice daily, for 10 days
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Result:Chronic Labetalol treatment significantly increased hypothalamic α1-receptor binding (+39%) and noradrenaline metabolism (MHPG/NA ratio +20%-100%) in neonatal rats, but did not induce long-term changes in adult receptor density.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 32780-64-6
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Appearance Solid
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분자량 364.87
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화학식 C19H25ClN2O3
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Color White to off-white
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SMILES
O=C(N)C1=CC(C(O)CNC(C)CCC2=CC=CC=C2)=CC=C1O.[H]Cl
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Synonyms
AH-5158 hydrochloride; Sch-15719W
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (5)
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Journal Impact Factor
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Most Recent
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J Med Chem
Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration. [Abstract]2021 Mar 11;64(5):2725-2738. PMID: 33619967 -
Eur J Pharmacol
The role of peripheral serotonin and norepinephrine in the gastroprotective effect against stress of duloxetine. [Abstract]2023 Feb 15:941:175499. PMID: 36627097
Labetalol hydrochloride purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2023 Feb 15:941:175499. [Abstract]
Labetalol (3-30 mg/kg; single dose) was intraperitoneally injected 0.5 h before water immersion restraint stress (WIRS). Labetalol dose-dependently prevented gastric ulcer.
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J Pharm Biomed Anal
Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. [Abstract]2021 Feb 20:195:113870. PMID: 33453569 -
Int J Clin Pract
Naringenin prevents pregnancy-induced hypertension via suppression of JAK/STAT3 signalling pathway in mice. [Abstract]2021 Oct;75(10):e14509. PMID: 34117816
용액&용해도
DMSO : ≥ 100 mg/mL (274.07 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 20 mg/mL (54.81 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.85 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.85 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
순도&문서
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Data Sheet (276 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Greenslade FC, et al. Labetalol binding to specific alpha- and beta-adrenergic sites in vitro and its antagonism of adrenergic responses in vivo. J Mol Cell Cardiol. 1979 Aug;11(8):803-11. [Content Brief]
[2]. Erdtsieck-Ernste EB, et al. Changes in adrenoceptors and monoamine metabolism in neonatal and adult rat brain after postnatal exposure to the antihypertensive labetalol. Br J Pharmacol. 1992 Jan;105(1):37-44. [Content Brief]
[3]. Johnson JD, et al. Catecholamines mediate stress-induced increases in peripheral and central inflammatory cytokines. Neuroscience. 2005;135(4):1295-307. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.7407 mL | 13.7035 mL | 27.4070 mL | 68.5176 mL |
| 5 mM | 0.5481 mL | 2.7407 mL | 5.4814 mL | 13.7035 mL | |
| 10 mM | 0.2741 mL | 1.3704 mL | 2.7407 mL | 6.8518 mL | |
| 15 mM | 0.1827 mL | 0.9136 mL | 1.8271 mL | 4.5678 mL | |
| 20 mM | 0.1370 mL | 0.6852 mL | 1.3704 mL | 3.4259 mL | |
| 25 mM | 0.1096 mL | 0.5481 mL | 1.0963 mL | 2.7407 mL | |
| 30 mM | 0.0914 mL | 0.4568 mL | 0.9136 mL | 2.2839 mL | |
| 40 mM | 0.0685 mL | 0.3426 mL | 0.6852 mL | 1.7129 mL | |
| 50 mM | 0.0548 mL | 0.2741 mL | 0.5481 mL | 1.3704 mL | |
| DMSO | 60 mM | 0.0457 mL | 0.2284 mL | 0.4568 mL | 1.1420 mL |
| 80 mM | 0.0343 mL | 0.1713 mL | 0.3426 mL | 0.8565 mL | |
| 100 mM | 0.0274 mL | 0.1370 mL | 0.2741 mL | 0.6852 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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