| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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| ln Vivo |
Subcutaneous injection of CX516 (10 and 20 mg/kg) markedly reduces certain extradimensional deficits caused by early postpartum or subchronic phencyclidine therapy [1].
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| Animal Protocol |
Animal/Disease Models: Male Lister Hooded rat (56-63 days after birth) [1]
Doses: 5, 10, 20 and 40 mg/kg Route of Administration: subcutaneous injection Experimental Results: Two doses (10 and 20 mg/kg) The improvement in extradimensional transformation defects caused by either treatment regimen is very significant. Two doses (5 and 40 mg/kg) were ineffective in reversing extradimensional damage induced by subchronic postpartum phencyclidine regimen. |
| References | |
| Additional Infomation |
CX-516 is a N-acylpiperidine.
Drug Indication Investigated for use/treatment in alzheimer's disease, memory loss, autism, neurologic disorders, dementia, schizophrenia and schizoaffective disorders, attention deficit/hyperactivity disorder (ADHD), and sleep disorders. Mechanism of Action CX 516 is a benzylpiperidine AMPAkine, an AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) modulator, that enhances the function of glutamate when it binds allosterically to the AMPA receptor channel complex. CX 516 slows receptor deactivation with a longer open time, slower excitatory postsynaptic potential (EPSP) decay and improvement of hippocampal long term potentiation (LTP). |
| Molecular Formula |
C14H15N3O
|
|---|---|
| Molecular Weight |
241.294
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| Exact Mass |
241.121
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| CAS # |
154235-83-3
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| Related CAS # |
CX516-d10;1286653-21-1
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| PubChem CID |
148184
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| Appearance |
White to light yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
433.1±25.0 °C at 760 mmHg
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| Melting Point |
88-90ºC
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| Flash Point |
215.8±23.2 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.640
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| LogP |
0.57
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
18
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| Complexity |
301
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ANDGGVOPIJEHOF-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C14H15N3O/c18-14(17-8-2-1-3-9-17)11-4-5-12-13(10-11)16-7-6-15-12/h4-7,10H,1-3,8-9H2
|
| Chemical Name |
piperidin-1-yl(quinoxalin-6-yl)methanone
|
| Synonyms |
BDP 12; BDP-12; CX-516; BDP12; SPD-420; CX 516; CX516; SPD420; brand name: Ampalex;
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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) |
H2O : ~100 mg/mL (~414.44 mM)
DMSO : ≥ 41 mg/mL (~169.92 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (11.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.75 mg/mL (11.40 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.75 mg/mL (11.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1444 mL | 20.7220 mL | 41.4439 mL | |
| 5 mM | 0.8289 mL | 4.1444 mL | 8.2888 mL | |
| 10 mM | 0.4144 mL | 2.0722 mL | 4.1444 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00001662 | COMPLETED | Drug: CX516 (Ampalex) | Alzheimer's Disease Dementia |
National Institute of Neurological Disorders and Stroke (NINDS) | 1996-12 | Phase 2 |
| NCT00235352 | COMPLETED | Drug: CX516 (Ampakine) | Schizophrenia | North Suffolk Mental Health Association | 2002-02 | Phase 2 Phase 3 |
| NCT00054730 | COMPLETED | Drug: CX516 (Ampalex®) | Autism Fragile X Syndrome |
RespireRx | 2002-06 | Phase 2 |
| NCT00040443 | COMPLETEDWITH RESULTS | Drug: CX516 Drug: Placebo |
Mild Cognitive Impairment | RespireRx | 2002-04 | Phase 2 |
| NCT00858689 | COMPLETEDWITH RESULTS | Drug: Minocycline | Fragile X Syndrome | FRAXA Research Foundation | 2007-10 | Not Applicable |
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