| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
BAN-ORL-24 HCl targets the NOP (nociceptin/orphanin FQ peptide) receptor, also known as opioid receptor-like 1 (ORL-1). It is a potent antagonist with an IC₅₀ of 0.27 nM for the NOP receptor. It shows high selectivity with IC₅₀ values of 2500 nM for κ-, 6700 nM for μ-, and >10000 nM for δ-opioid receptors.
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|---|---|
| ln Vitro |
BAN ORL 24 has NOR and MOR (opioid receptor subtype) antagonists with IC50 values of 50 μM and 0.224 μM respectively [2].
In vitro, BAN-ORL-24 HCl potently antagonizes the NOP receptor with an IC₅₀ of 0.27 nM. It shows high selectivity over κ-, μ-, and δ-opioid receptors. In a radioligand binding assay using CHO cell membranes expressing the human receptor, it has a Ki of 0.24 nM. |
| ln Vivo |
BAN ORL 24 (10 mg/kg; intravenously) attenuates the duration of BPRIM97 thermal analgesia [3]. Animal model: C57BL/6 mice [3] Dose: 10 mg/kg Administration dose: 10 mg/kg; iv results: Inhibited BPRIM97-induced analgesia 90 minutes after injection. BPR1M97-induced analgesia was not attenuated in the tail-clip test after 30 minutes.
In vivo, BAN-ORL-24 HCl has been studied for its ability to restrain the reduction of locomotor motions. It penetrates the brain and modulates NOP receptor-mediated effects. It has been used as a tool to study the role of the NOP receptor in various physiological processes. |
| Enzyme Assay |
The in vitro receptor binding assay for BAN-ORL-24 HCl involves competition binding experiments using radiolabeled NOP ligands. Membranes from cells expressing the human NOP receptor are incubated with varying concentrations of BAN-ORL-24 HCl and a fixed concentration of radioligand. Ki and IC₅₀ values are calculated.
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| Cell Assay |
In vitro cell-based assays for BAN-ORL-24 HCl are performed using cells expressing the NOP receptor. Cells are treated with BAN-ORL-24 HCl, and NOP receptor-mediated signaling, such as inhibition of cAMP accumulation or calcium mobilization, is measured. The compound's antagonist activity is assessed by its ability to block nociceptin-induced responses.
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| Animal Protocol |
In vivo animal experiments for BAN-ORL-24 HCl have been conducted in rodent models. Animals are administered the compound via appropriate routes, and locomotor activity is measured. The compound's effects on NOP receptor-mediated behaviors, such as pain modulation and anxiety, are assessed.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of BAN-ORL-24 HCl have been characterized in preclinical species. It penetrates the brain. Detailed PK parameters such as half-life, clearance, and brain penetration are determined from plasma and brain concentration-time profiles.
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| Toxicity/Toxicokinetics |
Toxicological data for BAN-ORL-24 HCl are limited. In standard preclinical safety assessments, it would be evaluated for potential off-target effects and general toxicity. The compound is intended for research use only and not for therapeutic use in humans.
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| References |
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| Additional Infomation |
BAN-ORL-24 HCl is a selective NOP receptor antagonist that has been used as a tool to study the role of the nociceptin/orphanin FQ system. It has been investigated for its potential in treating neurological and psychiatric disorders. It has not been approved for clinical use.
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| Molecular Formula |
C27H37CL2N3O2
|
|---|---|
| Molecular Weight |
506.507585287094
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| Exact Mass |
505.226
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| Elemental Analysis |
C, 64.03; H, 7.36; Cl, 14.00; N, 8.30; O, 6.32
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| CAS # |
1401463-54-4
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| Related CAS # |
BAN ORL 24 free base; 475150-69-7
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| PubChem CID |
56840444
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
34
|
| Complexity |
612
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
O=C([C@@H]1N(CC2=CC=CC=C2)CCC1)NCCCN3CCC4(CC3)OCC5=C4C=CC=C5.[H]Cl.[H]Cl
|
| InChi Key |
NEEVITHVDIQNJY-KHZPMNTOSA-N
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| InChi Code |
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
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| Chemical Name |
(2R)-1-benzyl-N-(3-spiro[1H-2-benzofuran-3,4'-piperidine]-1'-ylpropyl)pyrrolidine-2-carboxamide;dihydrochloride
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| Synonyms |
BAN-ORL-24 HCl; BAN-ORL-24 dihydrochloride; BAN-ORL24; BAN-ORL 24; BANORL-24; BANORL 24; BANORL24; BAN ORL 24
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~200 mg/mL (~394.86 mM)
H2O : ~100 mg/mL (~197.43 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (9.87 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (9.87 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (9.87 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (197.43 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9743 mL | 9.8715 mL | 19.7429 mL | |
| 5 mM | 0.3949 mL | 1.9743 mL | 3.9486 mL | |
| 10 mM | 0.1974 mL | 0.9871 mL | 1.9743 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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