BAN ORL 24NOP receptor antagonist, potent and selective CAS# 475150-69-7 |
- MCOPPB trihydrochloride
Catalog No.:BCC4161
CAS No.:1108147-88-1
Quality Control & MSDS
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| Cas No. | 475150-69-7 | SDF | Download SDF |
| PubChem ID | 56840444 | Appearance | Powder |
| Formula | C27H37Cl2N3O2 | M.Wt | 506.51 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble in DMSO > 10 mM | ||
| Chemical Name | (2R)-1-benzyl-N-(3-spiro[1H-2-benzofuran-3,4'-piperidine]-1'-ylpropyl)pyrrolidine-2-carboxamide;dihydrochloride | ||
| SMILES | C1CC(N(C1)CC2=CC=CC=C2)C(=O)NCCCN3CCC4(CC3)C5=CC=CC=C5CO4.Cl.Cl | ||
| Standard InChIKey | NEEVITHVDIQNJY-KHZPMNTOSA-N | ||
| Standard InChI | InChI=1S/C27H35N3O2.2ClH/c31-26(25-12-6-17-30(25)20-22-8-2-1-3-9-22)28-15-7-16-29-18-13-27(14-19-29)24-11-5-4-10-23(24)21-32-27;;/h1-5,8-11,25H,6-7,12-21H2,(H,28,31);2*1H/t25-;;/m1../s1 | ||
| 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. | ||
BAN ORL 24 Dilution Calculator
BAN ORL 24 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.9743 mL | 9.8715 mL | 19.7429 mL | 39.4859 mL | 49.3574 mL |
| 5 mM | 0.3949 mL | 1.9743 mL | 3.9486 mL | 7.8972 mL | 9.8715 mL |
| 10 mM | 0.1974 mL | 0.9871 mL | 1.9743 mL | 3.9486 mL | 4.9357 mL |
| 50 mM | 0.0395 mL | 0.1974 mL | 0.3949 mL | 0.7897 mL | 0.9871 mL |
| 100 mM | 0.0197 mL | 0.0987 mL | 0.1974 mL | 0.3949 mL | 0.4936 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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BAN ORL24 is a selective inhibitor of NOP with pK(i) value of 9.62 [1].
NOP (nociceptin/orphanin FQ (N/OFQ) peptide receptor) is a G protein coupled receptor and plays an important role in regulating many brain activities[2].
BAN ORL24 is a potent NOP inhibitor and has the highest affinity compared with other NOP inhibitors. When tested with CHO (hNOP) cells, administration of BAN ORL24 showed high affinity to cell membrane and higher selective compared with classical opioid receptors [1]. In SG neuron heterologously expressing NOP receptors with an enhanced basal facilitation ratio, BAN ORL24 treatment for 50 seconds enhanced the Ca2+ current amplitude for both prepulse and postpulse [3].
In the mouse tail withdrawal assay, administration of BAN ORL24 (10 mg/kg) combined with N/OFQ (1 nmol) antagonized the pronociceptive and antinociceptive effects of given supraspinally and spinally, respectively. Under the same experimental conditions BAN ORL24 did not affect the antinociceptive action of 3 nmol endomorphin-1 injected intrathecally [1].
References:
[1].Fischetti, C., et al., Pharmacological characterization of the nociceptin/orphanin FQ receptor non peptide antagonist Compound 24. Eur J Pharmacol, 2009. 614(1-3): p. 50-7.
[2].Donica, C.L., et al., Cellular mechanisms of nociceptin/orphanin FQ (N/OFQ) peptide (NOP) receptor regulation and heterologous regulation by N/OFQ. Mol Pharmacol, 2013. 83(5): p. 907-18.
[3].Mahmoud, S., et al., Modulation of silent and constitutively active nociceptin/orphanin FQ receptors by potent receptor antagonists and Na+ ions in rat sympathetic neurons. Mol Pharmacol, 2010. 77(5): p. 804-17.
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