TRPC5-IN-7
TRPC5-IN-7 is an orally active TRPC5 inhibitor (hTRPC5: IC50 = 0.77 μM). TRPC5-IN-7 inhibits the TRPC5 cation channel and TRPC5-mediated calcium influx by binding to the VSLD allosteric pocket, with selectivity for TRPC5 over TRPC3 and TRPC6. TRPC5-IN-7 exerts anxiolytic effects in mice and can be used for anxiety research.
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- Formule: C22H15F3N2O2
- Masse moléculaire:396.36
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
hTRPC5 0.77 μM (IC50) |
TRPC3 |
TRPC6 |
In Vitro
TRPC5-IN-7 (compound 9A1) (10 μM; 24-48 h post-transfection) inhibits hTRPC5 in HEK293T cells with an IC50 of 0.77 μM[1].
TRPC5-IN-7 (24-48 h after transfection) moderately inhibits hTRPC4 currents in HEK293T cells, with no significant inhibitory effect on hTRPC3 or hTRPC6[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 6-8 weeks old)[1]
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Dosage:10 mg/kg
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Administration:i.g.; once daily; days 1-8
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Result:Results from the open field test indicated that, compared to the control group, mice in the 9A1 and 11B1 groups exhibited more dense locomotor trajectories, demonstrating superior anxiolytic effects.
Analysis of distance traveled and time spent in the central area of the open field revealed that 9A1 significantly improved anxiety-related behaviors compared to the control group, exhibiting marked anxiolytic effects.
Results from the elevated plus maze test showed that, compared to the control group, mice in the HC-070 and 9A1 groups exhibited significantly increased entries into the open arms.
Subsequent analysis of dwell time and entry frequency revealed that the 9A1 group exhibited longer dwell time in the open arms, demonstrating the most pronounced anxiolytic effect.
Chemical Information
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Masse moléculaire 396.36
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Formule C22H15F3N2O2
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SMILES
FC(C=CC=C1)=C1CN2C(C(NC3=CC=C(F)C=C3O)=O)=CC4=C2C=CC(F)=C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TRPC5-IN-7 Related Classifications
HY-189736 Related Classifications
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