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Chemical Structure| 1628287-16-0 Chemical Structure| 1628287-16-0

Structure of Pico145
CAS No.: 1628287-16-0

Chemical Structure| 1628287-16-0

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Pico145 is a potent inhibitor of TRPC1/TRPC4/TRPC5 channels with IC50 values of 0.349 nM and 1.3 nM, respectively, widely used to study the role of transient receptor potential (TRP) channels in cellular signaling.

Synonyms: HC-608; Zerencotrep

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Cat. No.: {[proInfo.prAm]} Purity: {[proInfo.pro_purity]}

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Product Details of Pico145

CAS No. :1628287-16-0
Formula : C23H20ClF3N4O5
M.W : 524.88
SMILES Code : O=C(N1CCCO)N(C)C2=C(N(CC3=CC=C(Cl)C=C3)C(OC4=CC=CC(OC(F)(F)F)=C4)=N2)C1=O
Synonyms :
HC-608; Zerencotrep
MDL No. :MFCD31657331
InChI Key :PRJHEJGMSOBHTO-UHFFFAOYSA-N
Pubchem ID :85473438

Safety of Pico145

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Cortical neurons 200 nM 15 min Blocks the NCAM antibody-triggered increase in Fluo-4 AM signal intensity Int J Mol Sci. 2022 Sep 2;23(17):10027
Mouse CA1 pyramidal cells 100 nM 15-30 minutes To test the inhibitory effect of Pico145 on cholinergically induced persistent firing. In five out of six cells, persistent firing was completely blocked, and in the remaining cell, persistent firing was strongly reduced. Cells. 2020 Feb 5;9(2):365
Hippocampal neurons 1 nM 40 minutes Inhibition of TRPC1/4/5 channels, mimicking the effects of TRPC1 genetic depletion on synaptic plasticity. Front Cell Neurosci. 2018 Sep 14;12:318

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Morris Water Maze test Intraperitoneal injection 0.1 mg/kg Injected one hour before each probe test, for 5 days To evaluate the effect of Pico145 on spatial memory extinction, results showed that Pico145 significantly impaired memory extinction. Int J Mol Sci. 2020 Mar 3;21(5):1712
Mice Trpc1 knockout mice Brain slice perfusion 1 nM Single administration, lasting 40 minutes To investigate the role of TRPC1 in synaptic plasticity and spatial working memory. Pico145 inhibited TRPC1/4/5 channels, mimicking the effects of TRPC1 genetic depletion on LTP and LTD. Front Cell Neurosci. 2018 Sep 14;12:318
Mice Wild-type and NCAM-deficient mice In vitro culture 200 nM Single treatment, 15 min Reduces the NCAM-stimulated Ca2+ response and neurite outgrowth Int J Mol Sci. 2022 Sep 2;23(17):10027

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.91mL

0.38mL

0.19mL

9.53mL

1.91mL

0.95mL

19.05mL

3.81mL

1.91mL

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

References

 

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