Art. -Nr.: HY-171844

CX1739

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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.

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Reinheit: 99.63%
CAS. Nr.: 1086377-48-1
Formel: C₁₃H₁₅N₃O₃
Molecular Weight:261.28

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

CX1739 Chemical Structure

CAS. Nr.: 1086377-48-1

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Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle iGluR Isoform-spezifische Produkte anzeigen :

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	AUC_0-t	AUC_0-∞	T_1/2	T_max	C_max	AUC_0-∞ (Brain)	T_1/2 (Brain)	T_max (Brain)	C_max (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.

Chemical Information

CAS. Nr. 1086377-48-1
Appearance Solid
Molecular Weight 261.28
Formel C₁₃H₁₅N₃O₃
Color Light yellow to yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.8273 mL

19.1366 mL

38.2731 mL

5 mM

0.7655 mL

3.8273 mL

7.6546 mL

10 mM

0.3827 mL

1.9137 mL

3.8273 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Radin, D.P., et al. Low-Impact Ampakine CX1739 Exerts Pro-Cognitive Effects and Reverses Opiate-Induced Respiratory Depression in Rodents. Future Pharmacol. 2024, 4, 173-187.

[2]. Xiao D, et al. The impact and mechanism of ampakine CX1739 on protection against respiratory depression in rats. Future Med Chem. 2020;12(23):2093-2104. [Content Brief]

[3]. Fusco AF, et al. Acute Administration of Ampakine CX1739 after Cervical Spinal Cord Injury. J Neurotrauma. Published online October 6, 2025. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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CX1739

Immunology/Inflammation Compound Library

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

CNS-Penetrant Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle iGluR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CX1739

Immunology/Inflammation Compound Library

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

CNS-Penetrant Compound Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle iGluR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CX1739 Related Classifications

HY-171844 Related Classifications