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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C22H15F3N2O2
- 分子量:396.36
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
hTRPC5 0.77 μM (IC50) |
TRPC3 |
TRPC6 |
体外実験
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.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL/6 (male, 6-8 weeks old)[1]
-
Dosage:10 mg/kg
-
Administration:i.g.; once daily; days 1-8
-
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.
化学情報
-
分子量 396.36
-
分子式 C22H15F3N2O2
-
SMILES
FC(C=CC=C1)=C1CN2C(C(NC3=CC=C(F)C=C3O)=O)=CC4=C2C=CC(F)=C4
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)