1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. iGluR
  3. CX1739

CX1739 is an orally active, blood-brain barrier permeable, low-efficacy AMPA-glutamate receptor (AMPAR) potentiator. CX1739 enhances excitatory neurotransmission by potentiating glutamate-induced excitatory currents and promoting in vivo long-term potentiation. CX1739 eliminates amphetamine-induced locomotor activity, reverses opioid-, pentobarbital- and ethanol-induced respiratory depression, and exerts pro-cognitive effects in animals. CX1739 impairs motor function recovery and increases the risk of post-injury complications. CX1739 can be used in research related to attention-deficit/hyperactivity disorder, dementia, respiratory depression and spinal cord injury.

For research use only. We do not sell to patients.

CX1739

CX1739 Chemical Structure

CAS No. : 1086377-48-1

Size Price Stock Quantity
Free Sample (0.1 - 0.2 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

View All iGluR Isoform Specific Products:

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CX1739 is an orally active, blood-brain barrier permeable, low-efficacy AMPA-glutamate receptor (AMPAR) potentiator. CX1739 enhances excitatory neurotransmission by potentiating glutamate-induced excitatory currents and promoting in vivo long-term potentiation. CX1739 eliminates amphetamine-induced locomotor activity, reverses opioid-, pentobarbital- and ethanol-induced respiratory depression, and exerts pro-cognitive effects in animals. CX1739 impairs motor function recovery and increases the risk of post-injury complications. CX1739 can be used in research related to attention-deficit/hyperactivity disorder, dementia, respiratory depression and spinal cord injury[1][2][3].

In Vitro

CX1739 binds to the GluA2 LBD-L483Y-N754S AMPA receptor subunit via weak nonpolar interactions[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics
Species Dose Route AUC0-t AUC0-∞ T1/2 Tmax Cmax AUC0-∞ (Brain) T1/2 (Brain) Tmax (Brain) Cmax (Brain)
Rat[2] 10 mg/kg i.v. 17.467 mg·h/L 17.568 mg·h/L 1.072 h 0.033 h 13.275 mg/L 9.679 mg·h/L 0.908 h 0.033 h 8.295 mg/L
In Vivo

CX1739 (1-3 mg/kg; i.p.; single administration) significantly promotes in vivo LTP induction in the hippocampus of Long-Evans rats, increasing the average peak amplitude of EPSP by 12% and 22%, respectively, compared with the vehicle control group[1].
CX1739 (0.03-0.1 mg/kg, intraperitoneal injection, administered twice: 20 minutes before T1 and 20 minutes before T2) enhances novel object recognition memory in adult Wistar rats[1].
CX1739 (0.03-1 mg/kg; i.p.; single administration) significantly reduces the number of arm entries required for SD rats to locate the third baited arm in the win-shift radial arm maze, indicating improved spatial/working memory[1].
CX1739 (4-10 mg/kg; i.p.; single dose) significantly improves attentional performance and reduces impulsive behavior in hooded Lister rats during the 5-choice serial reaction time task (5CSRTT)[1].
CX1739 (5.6-30 mg/kg; i.p.; single administration) significantly reduces amphetamine-induced hyperactivity in mice in a dose-dependent manner in vivo[1].
CX1739 (5-20 mg/kg; intravenous administration; single bolus dose) partially reverses alfentanil-induced respiratory depression in rats at a dose of 10 mg/kg, while it completely reverses such depression at a dose of 20 mg/kg[1].
CX1739 (30 mg/kg; intravenous injection; single administration) immediately reverses severe acute respiratory depression induced by the opioid agonist 030418, sodium pentobarbital, and ethanol in male SD rats, restoring their respiratory rate to normal levels[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Long-Evans (male, 250-350 g)[1]
Dosage: 1 mg/kg; 3 mg/kg
Administration: i.p.; single dose
Result: Increased mean peak EPSP amplitude by approximately 12% relative to vehicle at 20 min post-tetanic stimulation for the 1 mg/kg dose.
Increased mean peak EPSP amplitude by approximately 22% relative to vehicle at 20 min post-tetanic stimulation for the 3 mg/kg dose.
Did not significantly augment EPSPs before electrical stimulation.
Animal Model: Wistar (adult male, 2-3 months, ~230-320 g)[1]
Dosage: 0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg
Administration: i.p.; two doses: 20 min prior to T1 and 20 min prior to T2
Result: Increased the novel object recognition index significantly at 0.03 mg/kg and 0.1 mg/kg doses.
Tended to increase recognition memory but did not reach statistical significance at 0.3 mg/kg dose.
Animal Model: Sprague-Dawley (male, ~3 months, 310-345 g)[1]
Dosage: 0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg; 1.0 mg/kg
Administration: i.p.; single dose
Result: Reduced the number of arm entries before finding the third baited arm significantly at 0.3 mg/kg dose.
No other dose comparisons reached statistical significance.
Animal Model: hooded Lister (male, 250-310 g at study start)[1]
Dosage: 4 mg/kg; 10 mg/kg
Administration: i.p.; single dose
Result: Increased % correct responses, reduced % premature responses, and reduced correct response latency significantly at 4 mg/kg dose.
Increased % correct responses, reduced % premature responses, reduced correct response latency, and increased % omissions at 10 mg/kg dose.
Animal Model: CD1 (adult male, 2-3 months, 29-36 g)[1]
Dosage: 5.6 mg/kg; 10 mg/kg; 18 mg/kg; 30 mg/kg
Administration: i.p.; single dose
Result: Reduced amphetamine-induced locomotor activity in a dose-dependent manner.
Produced a statistically significant reduction at 18 mg/kg dose.
Produced a statistically significant reduction at 30 mg/kg dose.
Animal Model: Sprague-Dawley (male, 295-330 g)[1]
Dosage: 5 mg/kg; 10 mg/kg; 20 mg/kg
Administration: i.v.; single bolus dose
Result: Reversed alfentanil-induced respiratory depression in a dose-dependent manner.
Produced a partial reversal at 10 mg/kg dose.
Produced a full reversal of minute volume to baseline levels at 20 mg/kg dose.
Animal Model: Sprague-Dawley (SD) (male, 200-220 g, respiratory depression induced by intravenous opioid agonist 030418)[2]
Dosage: 30 mg/kg
Administration: i.v.; single dose
Result: Restored respiratory rate to normal levels.
Molecular Weight

261.28

Formula

C13H15N3O3

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC2=NON=C2C=C1)N(C)C3CCOCC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (382.73 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.8273 mL 19.1366 mL 38.2731 mL
5 mM 0.7655 mL 3.8273 mL 7.6546 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.57 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.57 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.9%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.8273 mL 19.1366 mL 38.2731 mL 95.6828 mL
5 mM 0.7655 mL 3.8273 mL 7.6546 mL 19.1366 mL
10 mM 0.3827 mL 1.9137 mL 3.8273 mL 9.5683 mL
15 mM 0.2552 mL 1.2758 mL 2.5515 mL 6.3789 mL
20 mM 0.1914 mL 0.9568 mL 1.9137 mL 4.7841 mL
25 mM 0.1531 mL 0.7655 mL 1.5309 mL 3.8273 mL
30 mM 0.1276 mL 0.6379 mL 1.2758 mL 3.1894 mL
40 mM 0.0957 mL 0.4784 mL 0.9568 mL 2.3921 mL
50 mM 0.0765 mL 0.3827 mL 0.7655 mL 1.9137 mL
60 mM 0.0638 mL 0.3189 mL 0.6379 mL 1.5947 mL
80 mM 0.0478 mL 0.2392 mL 0.4784 mL 1.1960 mL
100 mM 0.0383 mL 0.1914 mL 0.3827 mL 0.9568 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
CX1739
Cat. No.:
HY-171844
Quantity:
MCE Japan Authorized Agent: