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Labetalol (AH5158; Sch15719W) is a potent, competitive, dual antagonist for both selective alpha1-adrenergic and nonselective beta-adrenergic receptors with antihypertensive properties. Labetalol is applied to address hypertension. For long-term hypertension management, it can be taken orally or intravenously in cases of severe hypertension. Research indicates that common CYP2C19 polymorphisms influence labetalol pharmacokinetics in a significant way.
| Targets |
α1-adrenergic receptor; β-adrenoceptor
|
|---|---|
| ln Vitro |
Labetalol exhibits a higher affinity for β-primergic sites on guinea pig heart and lung membranes (IC50 values of 0.8 and 4.0 μM, correspondingly)[2]. Labetalol binds to the rabbit uterine membrane's α-primergic binding site. Labctalol's binding affinity to the cardiac membrane's β-binding site is 19 times greater than that of the myocardial membrane's α-binding site [2].
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| ln Vivo |
Labetalol (10 mg/kg; ih) passes through the blood-brain barrier and, 90 minutes after injection, reaches tissue levels of 2.1 ug/g in the brains of 10-day-old mice[4]. Labetalol (5.0 mg/kg; ip) Partially inhibits the tailshock stress cascade by circulating IL-1β and IL-6 [5].
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| References |
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| Molecular Formula |
C19H24N2O3
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|---|---|
| Molecular Weight |
328.4055
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| Exact Mass |
328.18
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| Elemental Analysis |
C, 69.49; H, 7.37; N, 8.53; O, 14.61
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| CAS # |
36894-69-6
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| Related CAS # |
Labetalol hydrochloride; 32780-64-6
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| Appearance |
Solid powder
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| SMILES |
CC(CCC1=CC=CC=C1)NCC(C2=CC(=C(C=C2)O)C(=O)N)O
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| InChi Key |
SGUAFYQXFOLMHL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H24N2O3/c1-13(7-8-14-5-3-2-4-6-14)21-12-18(23)15-9-10-17(22)16(11-15)19(20)24/h2-6,9-11,13,18,21-23H,7-8,12H2,1H3,(H2,20,24)
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| Chemical Name |
2-hydroxy-5-[1-hydroxy-2-(4-phenylbutan-2-ylamino)ethyl]benzamide
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| Synonyms |
Trandate; Labetalol; Normodyne; Apo-Labetalol; Albetol; Dilevalol
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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 (~380.6 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.33 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.33 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0450 mL | 15.2249 mL | 30.4497 mL | |
| 5 mM | 0.6090 mL | 3.0450 mL | 6.0899 mL | |
| 10 mM | 0.3045 mL | 1.5225 mL | 3.0450 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 |
| NCT05551104 | Recruiting | Drug: Oral Nifedipine Drug: Oral Labetalol |
Postpartum Complication Maternal Hypertension |
Loma Linda University | December 2023 | Not Applicable |
| NCT04298034 | Recruiting | Drug: Labetalol, Nifedipine | Preeclampsia Hypertension in Pregnancy |
Medical College of Wisconsin | July 17, 2020 | Phase 3 |
| NCT04755764 | Recruiting | Drug: Labetalol Drug: Atenolol Drug: Nifedipine |
Systolic Hypertension Pregnancy Related |
Marshall University | March 3, 2021 | N/A |
| NCT05309460 | Not yet recruiting | Drug: Labetalol Oral Tablet Drug: NIFEdipine ER |
Postpartum Preeclampsia Hypertension in Pregnancy |
Nebraska Methodist Health System |
June 6, 2022 | Phase 4 |
| NCT06093893 | Not yet recruiting | Drug: Dexmedetomidine Drug: Nicardipine |
Hypotensive Anesthesia Orthognathic Surgery |
Boston Medical Center | March 2024 | Phase 4 |
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