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Seletracetam lithium bromide (Ucb 44212 lithium bromide) 2024584-38-9

Seletracetam lithium bromide (Ucb 44212 lithium bromide) 2024584-38-9

CAS No.: 2024584-38-9

Seletracetam (Ucb 44212) lithium bromide is an analogue of the antiepileptic drug Levetiracetam. Seletracetam lithium br
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This product is for research use only, not for human use. We do not sell to patients.

Seletracetam (Ucb 44212) lithium bromide is an analogue of the antiepileptic drug Levetiracetam. Seletracetam lithium bromide is an SV2A modulator used in epilepsy research.

Physicochemical Properties


Molecular Formula C10H14BRF2LIN2O2
Molecular Weight 275.74
Exact Mass 318.036
CAS # 2024584-38-9
Related CAS # Seletracetam;357336-74-4;Seletracetam lithium
PubChem CID 168439705
Appearance Typically exists as solid at room temperature
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 5
Rotatable Bond Count 4
Heavy Atom Count 18
Complexity 329
Defined Atom Stereocenter Count 2
SMILES

[Li+].CC[C@@H](C(=O)N)N1C[C@@H](CC1=O)C=C(F)F.[Br-]

InChi Key JLPMYEPKIQRREQ-VJBFUYBPSA-M
InChi Code

InChI=1S/C10H14F2N2O2.BrH.Li/c1-2-7(10(13)16)14-5-6(3-8(11)12)4-9(14)15;;/h3,6-7H,2,4-5H2,1H3,(H2,13,16);1H;/q;;+1/p-1/t6-,7+;;/m1../s1
Chemical Name

lithium;(2S)-2-[(4S)-4-(2,2-difluoroethenyl)-2-oxopyrrolidin-1-yl]butanamide;bromide
HS Tariff Code 2934.99.9001
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)

Biological Activity


Targets IC50: SV2A[1]
ln Vitro In comparison to Levetiracetam (6.1), Seletracetam has a one-log-unit greater affinity (pKi=7.1) for the LEV-binding site[2]. In vitro, seletracetam lithium bromide suppresses intracellular Ca2+ accumulation and high-voltage-activated Ca2+ currents in rat cortical neurons [2]. The administration of seletracetam (1-10 μM) lithium bromide in rat hippocampus slices lowers the amplitude and repeated firing of population spikes elicited by a high K+/low Ca2+ concentration fluid (HKLCF)[3].
ln Vivo In fully corneally-kindled mice, elotracetam (intraperitoneal injection) lithium bromide exhibits strong protection against secondary generalized motor seizures (ED50 0.31 mg/kg). With an ED50 of 0.17 mg/kg, selenium (ip) protects against the development of clonic convulsions in mice that are vulnerable to audiogenic seizures[3]. Seletracetam (0.0074 mg/kg to 74 mg/kg; intraperitoneal injection) lithium bromide has a generally much more potent effect than previously observed for Levetiracetam[3]. It also increases the generalized seizure threshold current and decreases the duration of the after-discharge and the seizure severity observed at the after-discharge threshold current.
Animal Protocol Animal/Disease Models: Female Wistar rats (200-220 g) (Amygdala-kindled rats)[3]
Doses: 0.0074,7.4, 74 mg/kg
Route of Administration: intraperitoneal (ip) injection; 60 min before seizure threshold determination
Experimental Results: Markedly increased the generalized seizure threshold at all doses tested, with increases of 190% (0.0074 mg/kg), 302% (0.074 mg/kg), 429% (0.74 mg/ kg), 433% (7.4 mg/kg) and 679% (74 mg/kg).
References [1]. Pollard JR, et al. Seletracetam, a small molecule SV2A modulator for the treatment of epilepsy. Curr Opin Investig Drugs. 2008 Jan;9(1):101-7.
[2]. Martella G, et al. Seletracetam (ucb 44212) inhibits high-voltage-activated Ca2+ currents and intracellular Ca2+ increase in rat cortical neurons in vitro. Epilepsia. 2009 Apr;50(4):702-10.
[3]. Matagne A, et al. Profile of the new pyrrolidone derivative seletracetam (ucb 44212) in animal models of epilepsy. Eur J Pharmacol. 2009;614(1-3):30-37.

Solubility Data


Solubility (In Vitro) May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
Solubility (In Vivo) Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300:Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)

Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.6266 mL 18.1330 mL 36.2660 mL
5 mM 0.7253 mL 3.6266 mL 7.2532 mL
10 mM 0.3627 mL 1.8133 mL 3.6266 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.