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.
For research use only. We do not sell to patients.
- CAS No.: 925924-27-2
- Formula: C27H23ClFN5O3
- Molecular Weight:519.95
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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.
| Species | Dose | Route | Plasma Concentration | Brain Concentration |
|---|---|---|---|---|
| Rat[1] | 0.2 mg/kg | i.v. | 14.0 ng/mL | 13.2 ng/g |
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.
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Animal Model:Wister (male, 11 weeks old, castrated 7 days prior to testing)[1]
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Dosage:0.22 mg/kg (repeated 5 times, total 1.1 mg/kg)
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Administration:i.v.; 5 times at 10-minute intervals
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Result:Reduced plasma LH levels by 32% compared to vehicle control at 60 minutes post-administration.
Reduced plasma LH levels significantly at 180 minutes post-administration.
Chemical Information
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CAS No. 925924-27-2
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Molecular Weight 519.95
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Formula C27H23ClFN5O3
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SMILES
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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GPR54 antagonist-1 Related Classifications
HY-182421 Related Classifications
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