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Levetiracetam (UCB-L059) Calcium Channel Inhibitor

Cat.No.: S1356

Levetiracetam (UCB-L059, SIB-S1) is an anticonvulsant medication used to treat epilepsy and an agonist of muscarinic acetylcholine receptors (mAChR). This compound also modulates the presynaptic P/Q-type voltage-dependent calcium (Ca2+) channel.
Levetiracetam (UCB-L059) Calcium Channel Inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 170.21

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Quality Control

Batch: Purity: 99.98%
99.98

Chemical Information, Storage & Stability

Molecular Weight 170.21 Formula

C8H14N2O2

Storage (From the date of receipt)
CAS No. 102767-28-2 Download SDF Storage of Stock Solutions

Synonyms UCB-L059, SIB-S1 Smiles CCC(C(=O)N)N1CCCC1=O

Solubility

In vitro
Batch:

DMSO : 34 mg/mL (199.75 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 34 mg/mL

Ethanol : 34 mg/mL

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In vivo
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Mechanism of Action

Targets/IC50/Ki
Calcium channel
In vitro
Levetiracetam (UCB-L059) and related compounds bind to SV2A expressed in fibroblasts, indicating that SV2A is sufficient for its binding. This compound irreversibly inhibits the high-voltage-activated (HVA) calcium current by approximately 18% on the average in freshly isolated CA1 hippocampal neurons of rats. It selectively inhibits N-type Ca2+ channels of CA1 pyramidal hippocampal neurons. Levetiracetam also reverses the inhibitory effect of DMCM on GABA-elicited currents in hippocampal neurons.
In vivo
Levetiracetam (UCB-L059) (17 mg/kg) produces a potent suppression of sound-induced clonic convulsions in mice, and this protective effect is significantly abolished by co-administration of the beta-carboline FG 7142. It exerts potent anticonvulsant activity against both focal and secondarily generalized seizures in fully amygdala-kindled rats, i.e. , a model of temporal lobe epilepsy. This compound (13 mg/kg, 27 mg/kg or 54 mg/kg, i.p.) dose-dependently suppresses the increase in seizure severity and duration induced by repeated amygdala stimulation. It has a relatively short half-life (about 2-3 hours) in rats. Levetiracetam (5.4 mg/kg to 96 mg/kg i.p.) dose-dependently inhibits both wild running and tonic-clonic convulsions in the audiogenic-seizure prone rat. It markedly suppresses spontaneous spike-and-wave discharge (SWD) but leaves the underlying EEG trace normal in the GAERS model of petit mal epilepsy.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/9454787/
  • [5] https://pubmed.ncbi.nlm.nih.gov/8991787/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-10-24)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07220902 NOT_YET_RECRUITING
Severe Preeclampsia; Eclampsia Preeclampsia
Nebraska Methodist Health System
2026-01-01 PHASE3
NCT06442748 RECRUITING
Seizures; Brain Tumors; Antiepileptics; Levetiracetam
Tata Memorial Centre
2024-07-04 PHASE3
NCT07336992 NOT_YET_RECRUITING
Spontaneous Intracerebral Hemorrhage
Hospices Civils de Lyon
2026-10-02 PHASE3
NCT07758062 NOT_YET_RECRUITING
Glioblastoma
Tianjin Medical University General Hospital
2026-09-01 PHASE2
NCT06907173 RECRUITING
Status Epilepticus
University of Virginia
2026-03-06 PHASE3
NCT07130786 RECRUITING
Seizures; Primary Motor Cortex; Brain Metastases From Non-small Cell Lung Cancer (NSCLC); Brain Metastases, Adult; Brain Metastases From Extra-cranial Solid Tumors
Ayal A. Aizer, MD
2025-12-23 PHASE2