| CAS NO: | 1094873-14-9 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 2mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| Molecular Weight (MW) | 565.68 |
|---|---|
| Formula | C34H36FN5O2 |
| CAS No. | 1094873-14-9 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO:>20 mg/mL |
| Water: <1 mg/mL | |
| Ethanol: <1 mg/mL | |
| SMILES | O=C(NC1=CC=C(N2CCN(C(C3=CC=CC=C3)C(N(CC)CC)=O)CC2)C(F)=C1)C4=CC=CC=C4C5=CC=CN=C5 |
| Synonyms | JNJ 31020028; JNJ31020028; JNJ-31020028; Chemical Name: N-(4-(4-(2-(diethylamino)-2-oxo-1-phenylethyl)piperazin-1-yl)-3-fluorophenyl)-2-(pyridin-3-yl)benzamide Exact Mass: 565.2853 |
| In Vitro | In vitro activity: JNJ-31020028 is a potent, selective and brain penetrant small molecule antagonist of the neuropeptide Y(2) receptor with pIC50=8.07 (human); pIC50=8.22 (rat); it is>100-fold selective versus human Y1/Y4/Y5 receptors. JNJ-31020028 bound with high affinity (pIC(50) = 8.07 +/- 0.05, human, and pIC(50) = 8.22 +/- 0.06, rat) and was>100-fold selective versus human Y(1), Y(4), and Y(5) receptors. JNJ-31020028 was demonstrated to be an antagonist (pK(B) = 8.04 +/- 0.13) in functional assays. JNJ-31020028 occupied Y(2) receptor binding sites (approximately 90% at 10 mg/kg) after subcutaneous administration in rats. JNJ-31020028 increased norepinephrine release in the hypothalamus, consistent with the colocalization of norepinephrine and neuropeptide Y. In a variety of anxiety models, JNJ-31020028 was found to be ineffective, although it did block stress-induced elevations in plasma corticosterone, without altering basal levels, and normalized food intake in stressed animals without affecting basal food intake. Kinase Assay: JNJ-31020028 was demonstrated to be an antagonist (pK(B) = 8.04 +/- 0.13) in functional assays. |
|---|---|
| In Vivo | JNJ-31020028 occupied Y(2) receptor binding sites (approximately 90% at 10 mg/kg) after subcutaneous administration in rats. JNJ-31020028 occupied Y(2) receptor binding sites (approximately 90% at 10 mg/kg) after subcutaneous administration in rats. Neither systemic (0, 15, 30, and 40 mg/kg, subcutaneously [s.c.]) nor intracerebroventricular (0.0, 0.3, and 1.0 nmol/rat) administration of JNJ-31020028 affected alcohol-reinforced lever pressing or relapse to alcohol seeking behavior following stress exposure. JNJ-31020028 (15 mg/kg, s.c.) did reverse the anxiogenic effects of withdrawal from a single bolus dose of alcohol on the elevated plus-maze, confirming the anxiolytic-like properties of NPY Y2 antagonism. Chronic administration of JNJ-31020028 induced a decrease in immobility time in the forced swim test in OBX while had no effect in control animals. |
| Animal model | Rats [olfactory bulbectomized (OBX) rat] |
| Formulation & Dosage | Dissolved in 20% 2-hydroxypropyl-beta-cyclodextrin for systemic treatment[2]; or dissolved in 1% DMSO and sterile saline for i.c.v. studies[2]; 0, 15, 30, and 40 mg/kg, subcutaneous |
| References | [1]. Psychopharmacology (Berl). 2010 Feb;208(2):265-77; [2]. Alcohol. 2011 Sep;45(6):567-76; [3]. Neuropeptides. 2012 Dec;46(6):329-34. |
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