GPR54 antagonist-1 

GPR54 antagonist‑1 is a GPR54 antagonist with IC₅₀ values of 3.6 nM and 15 nM against human and rat GPR54, respectively. GPR54 antagonist‑1 shows blood‑brain barrier penetration. GPR54 antagonist‑1 blocks the function of human and rat GPR54 receptors. GPR54 antagonist‑1 suppresses plasma luteinizing hormone levels in castrated male rats. GPR54 antagonist‑1 can be used for the study of prostate cancer and endometriosis^[1].

GPR54 antagonist-1 (compound 15a) (60 min) potently inhibits ¹²⁵I-metastin (40-54) binding to cell membranes expressing human or rat GPR54, with IC₅₀ values of 3.6 nM and 15 nM, respectively^[1].
GPR54 antagonist-1 fully inhibits metastin (40-54)-induced Ca²⁺ mobilization in human GPR54-expressing CHO cells with an IC₅₀ of 0.93 μM^[1].
GPR54 antagonist-1 (10 μM; 2 h) shows low P-glycoprotein-mediated efflux in Caco-2 monolayers^[1].

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

GPR54 antagonist-1 (compound 15a) (1.1 mg/kg; i.v.; 5 times at 10-minute intervals) suppresses plasma LH levels in castrated male rats^[1].
GPR54 antagonist-1 (0.2 mg/kg; i.v.; single dose) achieves a brain-to-plasma concentration ratio of 0.94 in male rats at 30 minutes post-dose^[1].

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

519.95

C₂₇H₂₃ClFN₅O₃

925924-27-2

N#CC1=C(C2=CC(N3CCNCC3)=CC=C2)C=C(C4=C(O)C=C(F)C=C4)N=C1NC(C5=CC=CO5)=O.Cl

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

• [1]. Kobayashi T, et al. 2-acylamino-4,6-diphenylpyridine derivatives as novel GPR54 antagonists with good brain exposure and in vivo efficacy for plasma LH level in male rats. Bioorg Med Chem. 2010;18(14):5157-5171.