1. GPCR/G Protein
    Neuronal Signaling
  2. Neuropeptide Y Receptor
  3. (R)-JNJ-31020028

(R)-JNJ-31020028 

Cat. No.: HY-107479
Handling Instructions

(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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(R)-JNJ-31020028 Chemical Structure

(R)-JNJ-31020028 Chemical Structure

CAS No. : 1094873-17-2

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Description

(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[1][2].

IC50 & Target[1]

human Y2 receptor

8.07 (pIC50)

rat Y2 receptor

8.22 (pIC50)

mouse Y2 receptor

8.21 (pIC50)

In Vivo

(R)-JNJ-31020028 (5.6 μg; chronic icv infusion; daily for 10 days) has antidepressant like effects in the olfactory bulbectomized rat (OBX) model[1].
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].

Animal Model: Male Sprague Dawley rats weighing 150-170 (OBX model)[1]
Dosage: 5.6 μg
Administration: chronic icv infusion; daily for 10 days
Result: Reduced OBX rat immobility time.
Animal Model: male Sprague-Dawley rat[2]
Dosage: 10 mg/kg
Administration: s.c. (Pharmacokinetic Analysis)
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.
Molecular Weight

565.68

Formula

C₃₄H₃₆FN₅O₂

CAS No.

1094873-17-2

SMILES

O=C(N(CC)CC)[[email protected]@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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Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

(R)-JNJ-31020028Neuropeptide Y ReceptorNPY receptorselectiveaffinityanti-depressantbehaviorsblood-brainbarrierCNSInhibitorinhibitorinhibit

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