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CX717

Alias: Ampakine CX-717 Ampakine CX717 Ampakine CX 717 CX 717 CX717 CX-717
Cat No.:V5669 Purity: ≥98%
CX 717 is a positive allosteric modulator (PAM) of the AMPA receptor.
CX717
CX717 Chemical Structure CAS No.: 867276-98-0
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
CX 717 is a positive allosteric modulator (PAM) of the AMPA receptor. Has antidepressant-like effects. Can be used for research on adult attention deficit hyperactivity disorder (ADHD).
Biological Activity I Assay Protocols (From Reference)
ln Vivo
Intracortical infusion of CX 717 (CX717; 20 mg/kg) increases the efflux of norepinephrine, dopamine, and serotonin, but not glutamate. CX 717 also produces a rapid (up to 1 hour) increase in brain-derived neurotrophic factor (BDNF) and a more sustained (up to 6 hours) increase in p11 [2]. CX 717 (CX717; 20 mg/kg) has fast (30 minutes) but transient (up to 24 hours) antidepressant-like effects in the forced swim test.
Animal Protocol
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats, body weight 280-350 g[2]
Doses: 20 mg/kg (administered as 1 mL/kg)
Route of Administration: intraperitoneal (ip) injection
Experimental Results: Induced antidepressant-like effects (20 mg/kg, ip) does not alter extracellular concentrations of norepinephrine (NA), dopamine (DA), serotonin (5-HT), and glutamate in the medial prefrontal cortex (mPFC).
References

[1]. Facilitation of task performance and removal of the effects of sleep deprivation by an ampakine (CX717) in nonhuman primates. PLoS Biol. 2005 Sep;3(9):e299.

[2]. Antidepressant-Like Effects of CX717, a Positive Allosteric Modulator of AMPA Receptors. Mol Neurobiol. 2020 Aug;57(8):3498-3507.

Additional Infomation
CX-717 is an ampakine compound previously investigated for the treatment of Attention-Deficit/Hyperactivity Disorder (ADHD) and Alzheimer's disease.
Drug Indication
Investigated for the treatment of Attention-Deficit/Hyperactivity Disorder (ADHD) and Alzheimer's disease.
Mechanism of Action
CX-717 is an ampakine compound. It is a positive allosteric modulator of AMPA receptors. Its action is theorized to be due to the facilitation of transmission at cortical synapses that use glutamate as a neurotransmitter. This in turn may promote plasticity at the synapse, which could translate into better cognitive performance. CX-717 works by allosterically binding to particular receptors in the brain, called AMPA-type glutamate receptors. This boosts the activity of glutamate, a neurotransmitter, and makes it easier to encode memory and to learn. In addition, CX717 could potentially strongly impact the up-regulation of BDNF (brain-derived neurotrophic factor) or NGF (nerve growth factor), two growth factors known to stimulate the formation of new circuitry in the brain associated with forming memory and cognition.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C11H11N3O3
Molecular Weight
233.23
Exact Mass
233.08
CAS #
867276-98-0
PubChem CID
3323368
Appearance
White to off-white solid powder
Density
1.4±0.1 g/cm3
Boiling Point
422.1±55.0 °C at 760 mmHg
Flash Point
209.1±31.5 °C
Vapour Pressure
0.0±1.0 mmHg at 25°C
Index of Refraction
1.623
LogP
-0.64
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
5
Rotatable Bond Count
1
Heavy Atom Count
17
Complexity
294
Defined Atom Stereocenter Count
0
InChi Key
KFRQROSRKSVROW-UHFFFAOYSA-N
InChi Code
InChI=1S/C11H11N3O3/c15-11(14-3-5-16-6-4-14)8-1-2-9-10(7-8)13-17-12-9/h1-2,7H,3-6H2
Chemical Name
2,1,3-benzoxadiazol-5-yl(morpholin-4-yl)methanone
Synonyms
Ampakine CX-717 Ampakine CX717 Ampakine CX 717 CX 717 CX717 CX-717
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

Note: This product requires protection from light (avoid light exposure) during transportation and storage.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~50 mg/mL (~214.39 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.72 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 25.0 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: ≥ 2.5 mg/mL (10.72 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 25.0 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.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (10.72 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 4.2876 mL 21.4381 mL 42.8761 mL
5 mM 0.8575 mL 4.2876 mL 8.5752 mL
10 mM 0.4288 mL 2.1438 mL 4.2876 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.

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03375021 COMPLETED Drug: CX717 200 mg
Drug: CX717 800 mg
Drug: Placebo
Attention Deficit Hyperactivity Disorder RespireRx 2005-07-19 Phase 2
Biological Data
  • DMS Performance and Match Response Latency under Normal Vehicle and Normal + CX717 Conditions (A) Normal vehicle condition, mean (± SEM) percent correct DMS performance across 11 monkeys. Each curve reflects percent correct DMS trials sorted by number of images (two to six) in the match phase on trials with different delays (1–30 s plotted in 5-s increments). Performance decreased both as a function of delay and number of images as indicated by separation of curves across delays. “C” on y-axis indicates random or “chance” performance level in task. Asterisks indicate degree of separation from 1–5 s delay trials for significant (*p < 0.01, **p < 0.001) differences, and daggers indicate minimum degree of separation for significance (†p < 0.01, ††p < 0.001) compared to two-image trials. (B) Match phase response latencies in s (mean ± SEM) for trials shown in (A). Latencies on correct trials were sorted and plotted by number of images at specified delays. Asterisks indicate significant differences (*p < 0.01, **p < 0.001) compared to the mean of two-image trials summed across all delays (dashed line).[1].Linda J Porrino, et al. Facilitation of task performance and removal of the effects of sleep deprivation by an ampakine (CX717) in nonhuman primates. PLoS Biol. 2005 Sep;3(9):e299.
  • Effects of Different Doses of CX717 on DMS Performance in Normal + CX717 Condition (A) CX717 is shown administered on consecutive sessions for nine monkeys over three dose ranges of CX717 (0.3–0.5 mg/kg, 0.8–1.0 mg/kg, and 1.5 mg/kg, IV). Each CX717 session (C, arrows) was interspersed with a single normal vehicle (V) session. Curves show mean (± SEM) percent correct performance over the entire session from each different monkey, as indicated by separate symbols. Arrows indicate CX717 sessions (also denoted by “C” on axis). Note escalating doses (0.3, 0.8, and 1.5 mg/kg) shown were in four of the nine monkeys. (B) Performance on split sessions (n = 4 monkeys) in which vehicle was administered at the start of the DMS session, and midway through same session CX717 (0.8 mg/kg, IV) was administered via remote pump without interruption. Mean (± SEM) percent correct performance over at least 50 trials was calculated separately for the first half (vehicle) and second half (CX717, 0.8 mg/kg) of the same session. Asterisks indicate a significant (** p < 0.001) increase in the second half of the session relative to the first (vehicle).[1].Linda J Porrino, et al. Facilitation of task performance and removal of the effects of sleep deprivation by an ampakine (CX717) in nonhuman primates. PLoS Biol. 2005 Sep;3(9):e299.
  • Effects of Sleep Deprivation and Sleep Deprivation + CX717 (A) Sleep deprivation condition disrupts DMS performance. Mean percent correct performance across animals for sessions following 30–36 h of sleep deprivation (nine of 11 monkeys in Figure 2A). Plus signs indicate significant mean differences (+ p < 0.01, ++ p < 0.001) compared to the respective number of images curve in the normal vehicle condition; dashed line at 60% allows comparison with Figure 2A. (B) Match response latencies in s (mean ± SEM) sorted for different trial types as in Figure 2B. Asterisks indicate significant difference (*p < 0.01, **p < 0.001) at all delays compared to two-image trials. Plus signs indicate significant differences (+ p < 0.01, ++ p < 0.001) compared to same trial types, and dashed line allows comparison with minimum latencies in normal vehicle condition (Figure 2B). (C) Sleep deprivation + CX717 condition. Effects of administration of CX717 (0.8 mg/kg, IV) 10 min prior to DMS session following 30–36 h of sleep deprivation. Mean (± SEM) percent correct DMS trials for same delay (1–30 sec, in 5-s increments) and #image (two to six) DMS conditions generated by same monkeys tested in (A). Plus signs indicate significant mean differences (+ p < 0.01, ++ p < 0.001) compared to the respective number of images curve in the normal vehicle condition (Figure 2A); pound signs (# p < 0.01,## p < 0.001) indicate significant differences compared to the same trial types in sleep deprivation condition. Dashed reference line allows comparison with sleep deprivation (A) and normal vehicle conditions (Figure 2A).[1].Linda J Porrino, et al. Facilitation of task performance and removal of the effects of sleep deprivation by an ampakine (CX717) in nonhuman primates. PLoS Biol. 2005 Sep;3(9):e299.
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