| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| 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. |
| 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)
|
| 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
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] 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). View More
Oral Formulation 3: Dissolved in PEG400 (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.
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.
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