| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C34H36FN5O2 |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
(R)-JNJ-31020028 is a high-affinity, selective, brain-penetrant antagonist of the neuropeptide Y Y2 receptor, with pIC50 values of 8.07, 8.22 and 8.21 for the human, rat, and mouse Y2 receptors, respectively. It shows more than 100-fold selectivity over the human Y1, Y4, and Y5 receptors and has antidepressant-like effects[1][2]. It has the molecular formula C34H36FN5O2 and a molecular weight of 565.68 g/mol.
Physical & Chemical Properties
| CAS Number | 1094873-17-2 |
|---|---|
| Molecular Formula | C34H36FN5O2 |
| Molecular Weight | 565.68 g/mol |
| 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 |
| Target | human Y 2 receptor, rat Y 2 receptor, mouse Y 2 receptor |
| Signaling Pathway | GPCR/G Protein; Neuronal Signaling |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
human Y2 receptor 8.07 (pIC50) |
rat Y2 receptor 8.22 (pIC50) |
mouse Y2 receptor 8.21 (pIC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vivo
In the olfactory bulbectomized rat (OBX) model, (R)-JNJ-31020028 (5.6 μg; chronic icv infusion; daily for 10 days) shows antidepressant like effects[1]. Chronic icv administration of (R)-JNJ-31020028 at 5.6 μg/day through an osmotic Alzet pump results in a significant decrease in the number of grooming events[1]. (R)-JNJ-31020028 treatment gives Cmax, Tmax, AUCinf, Vd, and t1/2 values of 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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