FMJ-01-054 

FMJ-01-054 is a selective dopamine D4 Receptor (D4R) antagonist with a K_i od 77.7 nM. FMJ-01-054 shows subtype selectivity over D2R and D3R. FMJ-01-054 inhibits D4R-mediated β-arrestin recruitment and cAMP production with IC₅₀ values of 3800 nM and 134 nM, respectively. FMJ-01-054 has desirable plasma half-life and brain exposure in rats. FMJ-01-054 can be used for the research of neurological disorders^[1].

FMJ-01-054 (compound 17) (0.3 nM-100 μM; 1 h) binds to the human dopamine D₄ receptor with high affinity (K_i = 77.7 nM) and >1287-fold selectivity over D₂ and D₃ receptors^[1].
FMJ-01-054 acts as an antagonist at the human dopamine D₄ receptor with an IC₅₀ of 3800 nM and has no agonist activity^[1].
FMJ-01-054 (30 min) inhibits dopamine D₄ receptor-mediated cAMP production as an antagonist with an IC₅₀ of 134 nM^[1].
FMJ-01-054 exhibits metabolic stability in rat and human liver microsomes with half-lives of 64.77 min and 46.84 min, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

FMJ-01-054 (compound 17) (5 mg/kg; i.p.; single dose) demonstrates adequate in vivo pharmacokinetic properties in Sprague−Dawley rats (with a plasma half-life of 2.10 hours, brain C_max of 3.04 nmol/g, and brain:plasma ratio of 0.30)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

368.86

C₁₉H₂₁ClN₆

CC1=CC(N2N=NC(CN3CCN(C4=NC=C(Cl)C=C4)CC3)=C2)=CC=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Mohammad Alkhatib, et al. Bioisosteric Replacement of Amides with 1,2,3-Triazoles Improves Dopamine D4 Receptor Ligand Pharmacokinetics. ACS Pharmacol. Transl. Sci. January 9, 2026.