BAN ORL 24 |
| Katalog-Nr.GC15926 |
A nociceptin receptor antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 475150-69-7
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 475150-69-7 | SDF | |
| Chemical Name | (2R)-1-benzyl-N-(3-spiro[1H-2-benzofuran-3,4'-piperidine]-1'-ylpropyl)pyrrolidine-2-carboxamide;dihydrochloride | ||
| Canonical SMILES | C1CC(N(C1)CC2=CC=CC=C2)C(=O)NCCCN3CCC4(CC3)C5=CC=CC=C5CO4.Cl.Cl | ||
| Formula | C27H37Cl2N3O2 | M.Wt | 506.51 |
| Löslichkeit | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.9743 mL | 9.8715 mL | 19.7429 mL |
| 5 mM | 394.9 μL | 1.9743 mL | 3.9486 mL |
| 10 mM | 197.4 μL | 987.1 μL | 1.9743 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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