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Chemical Structure| 1118460-77-7 Chemical Structure| 1118460-77-7

Structure of UCPH-101
CAS No.: 1118460-77-7

Chemical Structure| 1118460-77-7

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UCPH 101 selectively but not competitively inhibit excitatory amino acid transporter 1 (EAAT1) with IC50 of 660 nM. It exhibits relatively weak inhibition of other subtypes.

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Product Details of UCPH-101

CAS No. :1118460-77-7
Formula : C27H22N2O3
M.W : 422.48
SMILES Code : N#CC1=C(N)OC(CC(C2=C3C=CC=CC3=CC=C2)CC4=O)=C4C1C5=CC=C(OC)C=C5
MDL No. :MFCD12913298
InChI Key :YBMGNDPBARCLFT-UHFFFAOYSA-N
Pubchem ID :25223366

Safety of UCPH-101

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HEK293 cells 0.34 µM 6 minutes Investigate the inhibitory effect of UCPH-101 on EAAT1 J Neurosci. 2013 Jan 16;33(3):1068-87
Cortical pyramidal neurons (CPNs) 10 µM 15-18 minutes To evaluate the effect of GLAST inhibitor on the frequency of spontaneous excitatory postsynaptic currents (sEPSCs) in CPNs. Results showed that UCPH-101 did not significantly alter sEPSC frequency. CNS Neurosci Ther. 2019 Apr;25(4):509-518
Astrocyte-microglia-neuron mixed culture 0.1 to 10 µM 24 hours To evaluate the effect of UCPH-101 on L-glutamate uptake, it was found that UCPH-101 inhibited L-glutamate uptake in a concentration-dependent manner. J Neuroinflammation. 2012 Dec 23;9:275
HEK293T cells 200 µM 5 minutes To study the inhibitory effect of UCPH-101 on ASCT2, finding that it partially inhibits ASCT2's amino acid uptake activity. Elife. 2023 Mar 1;12:e83464
HEK293 cells 2 µM to 100 µM several seconds to minutes To investigate the non-competitive inhibitory mechanism of UCPH-101 on EAAT1, confirming that it inhibits EAAT1 activity by slowing substrate translocation rather than substrate or Na+ binding. Elife. 2023 Mar 1;12:e83464

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Male mice Fear conditioning model Bilateral BLA injection 10 nmol/μl Single injection, 30 minutes before training Inhibition of EAAT1 activity impaired long-term fear memory formation Commun Biol. 2024 Sep 17;7(1):1165

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.37mL

0.47mL

0.24mL

11.83mL

2.37mL

1.18mL

23.67mL

4.73mL

2.37mL

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

References

 

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