JNJ 5207787Selective NPY Y2 receptor antagonist CAS# 683746-68-1 |
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Quality Control & MSDS
3D structure
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| Cas No. | 683746-68-1 | SDF | Download SDF |
| PubChem ID | 10324083 | Appearance | Powder |
| Formula | C32H38N4O2 | M.Wt | 510.67 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 10 mM in DMSO with gentle warming and to 10 mM in ethanol with gentle warming | ||
| Chemical Name | (E)-N-(1-acetyl-2,3-dihydroindol-6-yl)-3-(3-cyanophenyl)-N-[1-(2-cyclopentylethyl)piperidin-4-yl]prop-2-enamide | ||
| SMILES | CC(=O)N1CCC2=C1C=C(C=C2)N(C3CCN(CC3)CCC4CCCC4)C(=O)C=CC5=CC=CC(=C5)C#N | ||
| Standard InChIKey | DSEJCLDJIFTPPH-FMIVXFBMSA-N | ||
| Standard InChI | InChI=1S/C32H38N4O2/c1-24(37)35-20-14-28-10-11-30(22-31(28)35)36(32(38)12-9-26-7-4-8-27(21-26)23-33)29-15-18-34(19-16-29)17-13-25-5-2-3-6-25/h4,7-12,21-22,25,29H,2-3,5-6,13-20H2,1H3/b12-9+ | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Selective NPY Y2 antagonist (IC50 = 0.1 μM). Displays 100-fold selectivity over NPY Y1, Y4 and Y5 receptors; also displays selectivity against a panel of 50 receptors, ion channels and transporters. Brain penetrant. |
JNJ 5207787 Dilution Calculator
JNJ 5207787 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.9582 mL | 9.7911 mL | 19.5821 mL | 39.1642 mL | 48.9553 mL |
| 5 mM | 0.3916 mL | 1.9582 mL | 3.9164 mL | 7.8328 mL | 9.7911 mL |
| 10 mM | 0.1958 mL | 0.9791 mL | 1.9582 mL | 3.9164 mL | 4.8955 mL |
| 50 mM | 0.0392 mL | 0.1958 mL | 0.3916 mL | 0.7833 mL | 0.9791 mL |
| 100 mM | 0.0196 mL | 0.0979 mL | 0.1958 mL | 0.3916 mL | 0.4896 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Characterization of N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyano-phenyl)-N-[1-(2-cyclopentyl-eth yl)-piperidin-4yl]acrylamide (JNJ-5207787), a small molecule antagonist of the neuropeptide Y Y2 receptor.[Pubmed:14617685]
J Pharmacol Exp Ther. 2004 Mar;308(3):1130-7.
The in vitro pharmacological properties of N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyano-phenyl)-N-[1-(2-cyclopentyl-eth yl)-piperidin-4yl]-acrylamide (JNJ-5207787), a novel neuropeptide Y Y(2) receptor (Y(2)) antagonist, were evaluated. JNJ-5207787 inhibited the binding of peptide YY (PYY) to human Y(2) receptor in KAN-Ts cells (pIC(50) = 7.00 +/- 0.10) and to rat Y(2) receptors in rat hippocampus (pIC(50) = 7.10 +/- 0.20). The compound was >100-fold selective versus human Y(1),Y(4), and Y(5) receptors as evaluated by radioligand binding. In vitro receptor autoradiography data in rat brain tissue sections confirmed the selectivity of JNJ-5207787. [(125)I]PYY binding sites sensitive to JNJ-5207787 were found in rat brain regions known to express Y(2) receptor (septum, hypothalamus, hippocampus, substantia nigra, and cerebellum), whereas insensitive binding sites were observed in regions known to express Y(1) receptor (cortex and thalamus). JNJ-5207787 was demonstrated to be an antagonist via inhibition of PYY-stimulated guanosine 5'-O-(3-[(35)S]thio)triphosphate binding ([(35)S]GTPgammaS) in KAN-Ts cells (pIC(50) corrected = 7.20 +/- 0.12). This was confirmed auto-radiographically in rat brain sections where PYY-stimulated guanosine 5'-O-(3-[(35)S]thio)triphosphate binding was inhibited by JNJ-5207787 (10 microM) in hypothalamus, hippocampus, and substantia nigra. After intraperitoneal administration in rats (30 mg/kg), JNJ-5207787 penetrated into the brain (C(max) = 1351 +/- 153 ng/ml at 30 min) and occupied Y(2) receptor binding sites as revealed by ex vivo receptor autoradiography. Hence, JNJ-5207787 is a potent and selective pharmacological tool available to establish the potential role of central and peripheral Y(2) receptors in vivo.
Novel non-peptidic neuropeptide Y Y2 receptor antagonists.[Pubmed:14980673]
Bioorg Med Chem Lett. 2004 Mar 8;14(5):1239-42.
Through SAR studies of a piperidinylindoline cinnamide HTS lead, the first potent, non-peptide, low molecular weight selective Neuropeptide Y Y2 (NPY Y2) antagonists have been synthesized. The SAR studies around the piperidinyl, the indolinyl, and the cinnamyl moieties are discussed.
