(R)-JNJ-31020028
(R)-JNJ-31020028 is a high affinity, selective brain penetrant neuropeptide Y Y2 receptor antagonist, with pIC50 values of 8.07, 8.22 and 8.21 for human, rat, and mouse Y2 receptor, respectively. (R)-JNJ-31020028 shows >100-fold selective versus human Y1, Y4, and Y5 receptors. (R)-JNJ-31020028 has antidepressant like effects.
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- CAS. Nr.: 1094873-17-2
- Formel: C34H36FN5O2
- Molecular Weight:565.68
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
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Help & FAQs
Alle Neuropeptide Y Receptor Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
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human Y2 receptor 8.07 (pIC50) |
rat Y2 receptor 8.22 (pIC50) |
mouse Y2 receptor 8.21 (pIC50) |
Chronic icv administration of (R)-JNJ-31020028 at 5.6 μg/day using osmotic Alzet pump resulted in a significant decreases number of grooming events[1].
(R)-JNJ-31020028 treatment shows the Cmax, Tmax , AUCinf, Vd, and t1/2 were 4.35 μM, 0.5 hours, 7.91 h μM and 0.83 hours, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague Dawley rats weighing 150-170 (OBX model)[1]
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Dosage:5.6 μg
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Administration:chronic icv infusion; daily for 10 days
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Result:Reduced OBX rat immobility time.
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Animal Model:male Sprague-Dawley rat[2]
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Dosage:10 mg/kg
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Administration:s.c. (Pharmacokinetic Analysis)
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Result:The Cmax, Tmax , AUCinf, Vd, and t1/2 were 4.35 μM, 0.5 hours, 7.91 h μM and 0.83 hours, respectively.
Chemical Information
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CAS. Nr. 1094873-17-2
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Molecular Weight 565.68
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Formel C34H36FN5O2
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SMILES
O=C(N(CC)CC)[C@@H](C1=CC=CC=C1)N2CCN(C3=CC=C(NC(C4=CC=CC=C4C5=CC=CN=C5)=O)C=C3F)CC2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Shoblock JR, et al. In vitro and in vivo characterization of JNJ-31020028 (N-(4-{4-[2-(diethylamino)-2-oxo-1-phenylethyl]piperazin-1-yl}-3-fluorophenyl)-2-pyridin-3-ylbenzamide), a selective brain penetrant small molecule antagonist of the neuropeptide Y [Content Brief]
[2]. Morales-Medina JC, et al. Chronic administration of the Y2 receptor antagonist, JNJ-31020028, induced anti-depressant like-behaviors in olfactory bulbectomized rat. Neuropeptides. 2012 Dec;46(6):329-34. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
(R)-JNJ-31020028 Related Classifications
HY-107479 Related Classifications
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