| Size | Price | |
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| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
AMPAR modulator-12 (compound K-4) (100 μM; 20–30 min after treatment) enhanced AMPA receptor-mediated evoked excitatory postsynaptic currents (EPSCs) in CA1 pyramidal neurons of the hippocampus, resulting in a significant increase in current amplitude relative to baseline levels [1]. AMPAR modulator-12 (0.1 μM) enhanced AMPA receptor-mediated evoked excitatory postsynaptic currents in pyramidal neurons of layers 2/3 of the barrel cortex [1].
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| ln Vivo |
AMPAR modulator-12 (1 mg/kg; intravenous injection; 7 days) exerted a rapid, AMPA receptor-dependent antidepressant-like effect in WKY rats [1]. AMPAR modulator-12 (1 mg/kg; intravenous injection; single dose) exerted a rapid antidepressant-like effect in a rat model of chronic restraint stress-induced depression [1].
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| Animal Protocol |
Animal/Disease Models:Wistar Kyoto (WKY) rats (male, 5-11 weeks old, congenital depression phenotype model)[1]
Doses: 1 mg/kg Route of Administration: Intravenous injection; single dose; once daily for 7 consecutive days Experimental Results: Compared with the control group, 3 hours after administration, immobility time in the forced swimming test (FST) was significantly reduced, tactile and feeding latency in the non-stimulatory feeding test (NSFT) was significantly shortened, and sucrose preference in the sucrose preference test (SPT) was increased. After 7 days of daily administration, immobility time in FST was significantly reduced on days 8 and 15 after drug withdrawal; this effect could be blocked by the AMPAR antagonist GYKI53655. On days 8 and 15 after drug withdrawal, sucrose preference was significantly increased in the SPT test; on day 22 after drug withdrawal, immobility time was significantly reduced in the FST test. There was no significant difference in motor activity compared to the vector control group. Thirty minutes after injection, compared to the vector control group, the mEPSC amplitude of pyramidal neurons in layers 2/3 of the mPFC was significantly restored, and the mEPSC frequency was significantly increased. After 7 days of daily administration followed by drug withdrawal, compared to the vector control group, the mEPSC and mIPSC amplitudes of pyramidal neurons in the mPFC were significantly increased, and the burst firing of neurons in the lateral habenula (LHb) was significantly reduced. Seven days after drug withdrawal, RNA sequencing results from mPFC tissue showed that Nox1 expression was downregulated by 2.61 times compared to the ketamine treatment group and by 2.28 times compared to intact rats. |
| References |
| Molecular Formula |
C19H22F2N2O4S2
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|---|---|
| Molecular Weight |
444.52
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| CAS # |
2163787-60-6
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
CN(C(COC1=C(C=C(C=C1F)SCCN(S(=O)(C2=CC=CC=C2)=O)C)F)=O)C
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| 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)
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| 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 | 2.2496 mL | 11.2481 mL | 22.4962 mL | |
| 5 mM | 0.4499 mL | 2.2496 mL | 4.4992 mL | |
| 10 mM | 0.2250 mL | 1.1248 mL | 2.2496 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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