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Chemical Structure| 215923-54-9 Chemical Structure| 215923-54-9

Structure of CX546
CAS No.: 215923-54-9

Chemical Structure| 215923-54-9

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CX-546 is a AMPAR potentiator which can destabilize the desensitized receptor conformation.

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Product Details of CX546

CAS No. :215923-54-9
Formula : C14H17NO3
M.W : 247.29
SMILES Code : O=C(C1=CC=C2OCCOC2=C1)N3CCCCC3
MDL No. :MFCD01860868
InChI Key :LJUNPHMOGNFFOS-UHFFFAOYSA-N
Pubchem ID :2890

Safety of CX546

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Primary cortical neurons 10 µM 2-4 days CX546 rescued the reduced responsiveness to NMDA and intracellular chloride levels. PMC8033520
Mecp2 null cortical neurons 20 µM 4 days CX546 rescued transcription of several genes, neuronal morphology, and responsiveness to stimuli. PMC8033520
Human ovarian cancer cell lines, OVCAR8 50-300 μM 72 hours To evaluate the effect of CX546 on cisplatin's anti-cancer efficacy. Co-treatment with 50 μM CX546 increased OVCAR8 cell viability by 10.79%, and 300 μM CX546 significantly increased SKOV3.ip1 cell viability by 30.48%. PMC11087041
Primary rat hippocampal neurons 50 μM 24 hours To evaluate the protective effect of CX546 against cisplatin-induced reduction in PSD-95 puncta density. CX546 significantly prevented cisplatin-induced reduction in PSD-95 puncta density. PMC11087041
Primary rat hippocampal neurons 50 μM 24 hours To evaluate the protective effect of CX546 against cisplatin-induced reduction in dendritic branching. CX546 significantly prevented cisplatin-induced reduction in dendritic arborizations. PMC11087041
Primary rat hippocampal neurons 50 μM 24 hours To evaluate the protective effect of CX546 against cisplatin-induced reduction in BDNF expression. CX546 alone significantly increased BDNF mRNA expression levels by ~6-fold and prevented cisplatin-induced reduction in BDNF levels. PMC11087041

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Rat paw incision (PI) model and spared nerve injury (SNI) model Intraperitoneal injection (systemic administration); Intra-NAc injection 2.5, 5, 10 mg/kg (systemic administration); 400, 800 μM/μl (intra-NAc administration) Single administration, analgesic effects lasted for 4 hours CX546 relieves mechanical hypersensitivity and depression-like behaviors associated with postoperative pain by activating AMPA receptors in the NAc PMC5226421
Mice Neonatal anesthesia model in mice Intraperitoneal injection 20 mg/kg Administered 1 hour after each anesthesia, repeated for 3 times CX546 enhances neuronal activity during the post-anesthesia recovery period, prevents long-term motor learning deficits, and ameliorates synaptic deficits. PMC5025762
Rats Neuropathic pain model (SNI) and inflammatory pain model (CFA) Intraperitoneal injection 5 mg/kg and 10 mg/kg Single administration, effects lasted 2-6 hours CX546 significantly reduced mechanical and cold allodynia in both SNI and CFA models and decreased immobility time in the forced swim test, indicating its analgesic and antidepressant effects. PMC4206834
Mecp2 null mice CD1 Mecp2tm1.1Bird RTT mouse model Subcutaneous injection 40 mg/kg Daily for 7 days CX546 prolonged lifespan, delayed disease progression, and rescued motor abilities and spatial memory. PMC8033520
Mice Neonatal mouse model Intraperitoneal injection 20 mg/kg Injected 1 hour after, continuous observation Potentiation of AMPA receptor function during emergence from anesthesia ameliorates neuronal dysfunction and prevents long-term behavioral deficits PMC8216302
Rats Chronic neuropathic pain model Intraperitoneal injection or direct infusion into PL-PFC 10 mg/kg (systemic) or 400 uM (intracranial) Single administration CX546 restored the anti-nociceptive response of PL-PFC neurons and inhibited symptoms of chronic pain PMC8126990
Mice Shank3B knockout mouse model Intraperitoneal injection 15 mg/kg Acute administration, 30 min before each behavioral test To evaluate the effects of CX546 on autism-relevant behavioral phenotypes in Shank3B mice. Results showed that CX546 significantly reduced self-grooming during the social interaction test in one cohort of Shank3B mice but had no significant effects on other social interaction parameters. PMC6402976
Mice Neto1-null mice Intraperitoneal injection 15 mg/kg Administered 30 min prior to each training session CX546 had no effect in wild-type mice but restored the deficits in LTP and spatial learning in Neto1-null mice PMC2652390
Mice Autism model Intraperitoneal or oral 25 mg/kg, 50 mg/kg, 75 mg/kg, 100 mg/kg Single acute dose CX546 reversed the deficit in sociability in BTBR mice on the most sensitive parameter, time spent sniffing a novel mouse as compared to time spent sniffing a novel object. PMC3445667
Rats Recognition memory tasks Local infusions 0.1 and 0.3 μg/μl 5 min delay phase CX546 had no effect on recognition memory performance PMC4854963

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.04mL

0.81mL

0.40mL

20.22mL

4.04mL

2.02mL

40.44mL

8.09mL

4.04mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.

References

 

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