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Levetiracetam (UCB-L059) Calcium Channel inhibitor

Name: Levetiracetam (UCB-L059)
Brand: Selleck Chemicals
SKU: S1356
Availability: InStock
Rating: 5 (6 reviews)

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.

Chemical Structure

Molecular Weight: 170.21

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	CD markers AChR Sodium Channel Potassium Channel GABA Receptor ATPase TRP Channel GluR NMDAR P2 Receptor Proton Pump P-gp CFTR SGLT Chloride Channel MCT Amino acid transporter GLUT CRM1 VDAC BCRP NKCC OCT NCX OAT VMAT Aquaporin EAAT GlyT GlyR
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Chemical Information, Storage & Stability

Molecular Weight	170.21	Formula	C₈H₁₄N₂O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	102767-28-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	UCB-L059, SIB-S1			Smiles	CCC(C(=O)N)N1CCCC1=O

Solubility

In vitro
Batch:

DMSO : 34 mg/mL ( (199.75 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 34 mg/mL

Ethanol : 34 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	Saline Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	30.000mg/ml (176.25mM)	Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Calcium channel ^[1]
In vitro	Levetiracetam (UCB-L059) and related compounds bind to SV2A expressed in fibroblasts, indicating that SV2A is sufficient for its binding. ^[1] 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. ^[2] Levetiracetam also reverses the inhibitory effect of DMCM on GABA-elicited currents in hippocampal neurons. ^[3]
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. ^[3] 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. ^[4] 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. ^[5]
References	https://pubmed.ncbi.nlm.nih.gov/15917812/ https://pubmed.ncbi.nlm.nih.gov/11879381/ https://pubmed.ncbi.nlm.nih.gov/12086975/ https://pubmed.ncbi.nlm.nih.gov/9454787/ https://pubmed.ncbi.nlm.nih.gov/8991787/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05860153	Not yet recruiting	Febrile Convulsion	Assiut University	June 1 2023	Not Applicable
NCT06403150	Enrolling by invitation	Status Epilepticus	Dhaka Medical College	May 15 2023	Phase 4
NCT06067412	Completed	Status Epilepticus	Shaheed Zulfiqar Ali Bhutto Medical University	August 1 2022	Not Applicable
NCT04425798	Unknown status	Glioma\|Epilepsy	Beijing Neurosurgical Institute\|Beijing Tiantan Hospital	May 25 2022	--
NCT04117425	Recruiting	Epilepsy in Pregnancy	Assistance Publique - Hôpitaux de Paris	April 20 2022	Not Applicable

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