Labetalol
Based on 5 publication(s) in Google Scholar
Labetalol (AH5158) is an orally available, selective α1-adrenergic recepto and non-selective β-adrenergic receptor competitive antagonist. Labetalol is an antihypertensive molecule that partially crosses the blood-brain barrier and has little effect on cardiac output. Labetalol can be used in the study of cardiovascular diseases, such as hypertension during pregnancy.
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- Pureza: 99.94%
- No. CAS: 36894-69-6
- Fòrmula: C19H24N2O3
- Peso molecular:328.41
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Labetalol
MoreVer todos los productos específicos de isoformas Adrenergic Receptor
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Actividad biológica
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α1-adrenergic receptor |
β-adrenoceptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
>100 μM
Compound: Labetalol
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Antiproliferative activity against human A375 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human A375 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
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[PMID: 32216987] |
| SK-MEL-28 | IC50 |
>100 μM
Compound: Labetalol
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Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
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[PMID: 32216987] |
| SK-MEL-5 | IC50 |
>100 μM
Compound: Labetalol
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Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human SK-MEL-5 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
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[PMID: 32216987] |
Labetalol 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 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) 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) 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 (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.
Chemical Information
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No. CAS 36894-69-6
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Appearance Solid
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Peso molecular 328.41
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Fòrmula C19H24N2O3
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Color White to off-white
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SMILES
O=C(C1=CC(C(CNC(CCC2=CC=CC=C2)C)O)=CC=C1O)N
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Synonyms
AH5158; Sch-15719W free base
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
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 -
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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 -
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
Solvente y solubilidad
DMSO : 100 mg/mL (304.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.33 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0450 mL | 15.2249 mL | 30.4497 mL | 76.1244 mL |
| 5 mM | 0.6090 mL | 3.0450 mL | 6.0899 mL | 15.2249 mL | |
| 10 mM | 0.3045 mL | 1.5225 mL | 3.0450 mL | 7.6124 mL | |
| 15 mM | 0.2030 mL | 1.0150 mL | 2.0300 mL | 5.0750 mL | |
| 20 mM | 0.1522 mL | 0.7612 mL | 1.5225 mL | 3.8062 mL | |
| 25 mM | 0.1218 mL | 0.6090 mL | 1.2180 mL | 3.0450 mL | |
| 30 mM | 0.1015 mL | 0.5075 mL | 1.0150 mL | 2.5375 mL | |
| 40 mM | 0.0761 mL | 0.3806 mL | 0.7612 mL | 1.9031 mL | |
| 50 mM | 0.0609 mL | 0.3045 mL | 0.6090 mL | 1.5225 mL | |
| 60 mM | 0.0507 mL | 0.2537 mL | 0.5075 mL | 1.2687 mL | |
| 80 mM | 0.0381 mL | 0.1903 mL | 0.3806 mL | 0.9516 mL | |
| 100 mM | 0.0304 mL | 0.1522 mL | 0.3045 mL | 0.7612 mL |
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