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Dopamine D3 receptor antagonist-3 is a selective positive allosteric modulator-antagonist (PAM-antagonist) of the D3 dopamine receptor (D3R) that can cross the blood-brain barrier. It demonstrates antagonistic activity in D3R-mediated β-arrestin recruitment assays with an IC50 of 2.5 μM and Kb of 0.49 μM, and in D3R-mediated Go-BRET assays with an IC50 of 0.34 μM. Dopamine D3 receptor antagonist-3 is applicable for the study of neuropsychiatric disorders, including substance use disorders.

| 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 | Dopamine D3 receptor antagonist-3 is a selective positive allosteric modulator-antagonist (PAM-antagonist) of the D3 dopamine receptor (D3R) that can cross the blood-brain barrier. It demonstrates antagonistic activity in D3R-mediated β-arrestin recruitment assays with an IC50 of 2.5 μM and Kb of 0.49 μM, and in D3R-mediated Go-BRET assays with an IC50 of 0.34 μM. Dopamine D3 receptor antagonist-3 is applicable for the study of neuropsychiatric disorders, including substance use disorders. |
| Targets&IC50 | Dopamine D3 receptor:0.49 μM (Kd) |
| In vitro | Dopamine D3 receptor antagonist-3 (Compound 6a) demonstrates excellent microsomal stability in humans, mice, and rats, and shows no activity against the hERG channel, with an IC50 value greater than 10 μM. |
| In vivo | Compound 6a, a dopamine D3 receptor antagonist, demonstrates brain permeability when administered at 40 mg/kg via intraperitoneal injection (single dose). It has a brain half-life of 3.65 hours and reaches a peak brain concentration (C maxs) of 3183 ng/g (6.5 μM). |
| Molecular Weight | 485.86 |
| Formula | C18H17ClF5N3O3S |
| Cas No. | 2894793-37-2 |
| Smiles | O=C(C1=C(NC(=C1S(=O)(=O)NC2=CC=C(C(Cl)=C2)C(F)(F)F)C)C)N3CCC(F)(F)C3 |
| 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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