| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
S-8510 has strong affinity for BDZ receptors. The ratio of the Ki value of each ligand with and without GABA is defined as the GABA ratio, which is regarded a biological indication of BDZ receptor ligands. The GABA ratio of S-8510 or CGS8216 is close to the value of flumazenil, which is considered an antagonist or a very weak agonist. S-8510 (10-7 M) improves LTP, and this enhancement is antagonized by the BDZ receptor antagonist flumazenil. Flumazenil alone does not impair LTP or elicit a reaction prior to tetanus challenge. S-8510 has no effect on field-evoked potentials up to 10-5 M. However, S-8510 increased the amplitude of population spikes at a dose of 10-4 M, and this action was entirely antagonized by concurrent application of flumazenil (10-4 M) [1].
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|---|---|
| ln Vivo |
Convulsions that are lethal only when S-8510 or CGS8216 are taken in excess of 90 mg/kg of PTZ. S-8510's proconvulsant action seems to be specific to subconvulsive states brought on by PTZ. Scopolamine may have amnestic effects since it decreased the amount of time spent in the vicinity of the platform. S-8510 and CGS8216 counteract amnesia brought on by scopolamine. S-8510 also improves memory impairment caused by diazepam in passive avoidance and water maze paradigms. ACh levels were raised by S-8510 in a dose-dependent manner to 100 mg/kg. Hippocampal extracellular NA levels were raised in a dose-dependent manner by both PTZ and S-8510. The water-licking conflict paradigm was used to investigate the anxiolytic effects of S-8510, CGS8216, and FG7142 in Wistar rats. Even at doses of up to 30 mg/kg, S-8510 and CGS8216 were unable to alter this behavioral trend. S-8510 dramatically shortened the duration of immobility in the forced swim test in ddY mice, with dosages ranging from 40 to 80 mg/kg. At doses more than 10 mg/kg, S-8510 dramatically decreased the degree of tetrabenazine-induced ptosis in the tetrabenazine-induced ptosis mouse. Similarly, imipramine was more successful (reducing ptosis by almost 80% at 20 mg/kg) than S-8510, which only decreased it by 39% even at the maximal dose [1].
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| References | |
| Additional Infomation |
S-8510 / SB-737552 is a BZD inverse agonist investigated for the treatment of Alzheimer’s disease and mild to moderate senile dementia. It was being codeveloped by Shionogi and GlaxoSmithKline.
Drug Indication Investigated for use/treatment in alzheimer's disease and dementia. Mechanism of Action S-8510 is a BZD partial inverse agonist to the BZD site on the GABA-A receptors in the central nervous system. As an inverse agonist (which as a group elicit CNS effects such as insomnia, agitation, and proconvulsant behaviors), S-8510 functions as a negative modulator of the GABA-A receptor. S-8510, however, is a partial inverse agonist, which means it has a lower affinity for the BZD binding site than do full agonists, and studies in animals have shown that the drug does not induce convulsions or anxiety. |
| Molecular Formula |
C12H10N4O2.H3O4P
|
|---|---|
| Molecular Weight |
340.22862
|
| Exact Mass |
340.057
|
| CAS # |
151466-23-8
|
| Related CAS # |
151224-83-8;151466-23-8 (phosphate);
|
| PubChem CID |
135484551
|
| Appearance |
Typically exists as solid at room temperature
|
| Boiling Point |
393.4ºC at 760 mmHg
|
| Flash Point |
191.7ºC
|
| Vapour Pressure |
2.14E-06mmHg at 25°C
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
23
|
| Complexity |
366
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=P(O)(O)O.C12=NC=C3C(NC(C4=NOC=C4)=N3)=C1COCC2
|
| InChi Key |
SMMFBCMFJOBTLP-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C12H10N4O2.H3O4P/c1-3-17-6-7-8(1)13-5-10-11(7)15-12(14-10)9-2-4-18-16-9;1-5(2,3)4/h2,4-5H,1,3,6H2,(H,14,15);(H3,1,2,3,4)
|
| Chemical Name |
4-(1,2-oxazol-3-yl)-12-oxa-3,5,8-triazatricyclo[7.4.0.02,6]trideca-1,3,6,8-tetraene;phosphoric acid
|
| 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)
|
| 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
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|---|---|
| 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 | 2.9392 mL | 14.6959 mL | 29.3919 mL | |
| 5 mM | 0.5878 mL | 2.9392 mL | 5.8784 mL | |
| 10 mM | 0.2939 mL | 1.4696 mL | 2.9392 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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