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Compound 6.4, also known as 5-HT7R antagonist 3, is a selective antagonist of the 5-HT7R with a Ki of 8 nM. It exhibits significantly less affinity towards D2R, 5-HT1AR, and 5-HT2AR with Ki values of 511 nM, 8930 nM, and 5786 nM, respectively. In mice, 5-HT7R antagonist 3 demonstrates anti-depressant and anti-anxiety activities.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | Compound 6.4, also known as 5-HT7R antagonist 3, is a selective antagonist of the 5-HT7R with a Ki of 8 nM. It exhibits significantly less affinity towards D2R, 5-HT1AR, and 5-HT2AR with Ki values of 511 nM, 8930 nM, and 5786 nM, respectively. In mice, 5-HT7R antagonist 3 demonstrates anti-depressant and anti-anxiety activities. |
| Targets&IC50 | D2 Receptor:511nM(ki), 5-HT7 Receptor:8nM(ki), 5-HT2A Receptor:5786nM(ki), 5-HT1A Receptor:8930nM(ki) |
| In vitro | 5-HT 7 R antagonist 3, active across a range of 1 pM to 1 μM, inhibits cAMP production in cells stably expressing human 5-HT, achieving an IC50 of 113 nM and a K_b of 14 nM. |
| In vivo | The compound 5-HT7R antagonist 3, administered intraperitoneally at doses of 1.25-10 mg/kg to male BalbC mice (20-25 g) 60 minutes before testing, exhibited significant anti-anxiety and antidepressant effects. |
| Molecular Weight | 516.61 |
| Formula | C30H33FN4O3 |
| Cas No. | 1887043-58-4 |
| Smiles | C(N1CCN(C[C@H](CN2C(=O)[C@@](C)(NC2=O)C3=CC=C(F)C=C3)O)CC1)(C4=CC=CC=C4)C5=CC=CC=C5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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