| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Ki: 1.8 nM (MOP), 4.2 nM (NOP)[1]
BPR1M97 targets both the mu opioid receptor (MOP) and the nociceptin-orphanin FQ peptide (NOP) receptor as a dual-acting agonist. It has Ki values of 1.8 nM for MOP and 4.2 nM for NOP. By activating both receptors, BPR1M97 produces potent antinociceptive and anti-hyperalgesic effects. The compound's blood-brain barrier permeability supports its central nervous system activity. Its bifunctional mechanism makes it a valuable tool for studying the interplay between MOP and NOP receptor signaling in pain modulation. |
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| ln Vitro |
In vitro, BPR1M97 is a dual-acting agonist at MOP and NOP receptors with Ki values of 1.8 nM and 4.2 nM, respectively. It has blood-brain barrier permeability and potency. The compound's high affinity for both receptors makes it a valuable research tool for studying opioid and nociceptin receptor pharmacology. Detailed in vitro characterization data, including receptor binding and functional assays, are available in the primary literature. The compound's bifunctional mechanism may offer advantages for pain research.
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| ln Vivo |
In a mouse model of cancer pain, BPR1M97 (1.8 mg/kg; sc; once) exhibits antinociception[1].
In vivo, BPR1M97 (1.8 mg/kg; s.c.; single dose) exhibits anti-hyperalgesic effects in mouse cancer pain models. As a dual MOP/NOP agonist with blood-brain barrier permeability, it produces potent antinociceptive and anti-hyperalgesic effects. The compound's efficacy in cancer pain models suggests potential applications in pain research. Specific in vivo efficacy data and detailed animal model studies are available in the primary literature. Further research is ongoing to characterize its full therapeutic potential for pain management. |
| Enzyme Assay |
For MOP and NOP receptor binding assays, membrane preparations from cells expressing recombinant MOP or NOP receptors are incubated with radiolabeled ligands and varying concentrations of BPR1M97. Non-specific binding is determined using excess unlabeled reference compounds. Following incubation at appropriate temperature (typically 25°C for 60-90 minutes), bound and free radioligands are separated by rapid filtration through glass fiber filters. Filters are washed and radioactivity counted by liquid scintillation. Ki values (1.8 nM for MOP, 4.2 nM for NOP) are calculated from competition curves. For functional assays, G protein activation is measured by [35S]-GTPγS binding.
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| Cell Assay |
For in vitro cellular assays, cell lines expressing MOP or NOP receptors (e.g., CHO or HEK293 cells) are cultured in appropriate media under standard conditions (37°C, 5% CO2). BPR1M97 is dissolved in DMSO and diluted in culture medium to desired concentrations. Cells are treated with compound for specified durations. Receptor activation is assessed by measuring downstream signaling (e.g., cAMP inhibition, calcium flux, or ERK phosphorylation). Cell viability and cytotoxicity can be assessed using standard assays. Each concentration is tested in replicate wells with vehicle controls and positive controls.
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| Animal Protocol |
Animal/Disease Models: Male wild-type C57BL/6 mice (25-30 g)[1]
Doses: 1.8 mg/kg Route of Administration: subcutaneous (sc) injection (sc); once Experimental Results: Demonstrated antinociception in a murine model of cancer pain. For in vivo animal studies, BPR1M97 is typically formulated in suitable vehicles and administered via subcutaneous (s.c.) injection. In mouse cancer pain models, a single dose of 1.8 mg/kg produces anti-hyperalgesic effects. Dosing regimens vary by study objective. Pain responses are assessed using standard nociceptive tests. Blood and tissue samples may be collected for pharmacokinetic analysis. All procedures must follow institutional animal care and use committee guidelines. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of BPR1M97 indicate it has blood-brain barrier permeability. The compound has a molecular weight of 349.25, formula C18H18Cl2N2O, and CAS number 2059904-66-2. Purity: 99.95%. Appearance: yellow solid. Storage: powder at -20°C for 3 years; in solvent at -80°C for 1 year. Solubility: DMSO 225 mg/mL (644.24 mM). In vivo formulation: 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% saline (5 mg/mL).
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| Toxicity/Toxicokinetics |
According to available safety information, BPR1M97 is intended for research purposes only and is not for human use. Standard laboratory safety precautions should be followed when handling this compound, including the use of appropriate personal protective equipment (gloves, lab coat, safety goggles). The compound should be handled in a well-ventilated area. Avoid dust formation and inhalation. In case of skin contact, wash with plenty of soap and water. In case of eye contact, rinse cautiously with water for several minutes. No clinical toxicity data are available.
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| References | |
| Additional Infomation |
BPR1M97 is a dual-acting MOP/NOP agonist with Ki values of 1.8 nM (MOP) and 4.2 nM (NOP). It has blood-brain barrier permeability and exhibits antinociceptive and anti-hyperalgesic effects. At 1.8 mg/kg s.c., it shows anti-hyperalgesic effects in mouse cancer pain models. It has a molecular weight of 349.25 and formula C18H18Cl2N2O. It is for research use only with no regulatory approvals reported.
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| Molecular Formula |
C18H18CL2N2O
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|---|---|
| Molecular Weight |
349.25
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| Exact Mass |
348.079
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| CAS # |
2059904-66-2
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| PubChem CID |
137541784
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| Appearance |
White to off-white solid powder
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| Density |
1.260±0.06 g/cm3(Predicted)
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| Boiling Point |
484.1±45.0 °C(Predicted)
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| LogP |
4.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
420
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1CCC2=CC=CC=C2C1CNC(=O)C3=CC(=C(C=C3)Cl)Cl
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| InChi Key |
LIYLICKKTYEDQP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H18Cl2N2O/c1-22-9-8-12-4-2-3-5-14(12)17(22)11-21-18(23)13-6-7-15(19)16(20)10-13/h2-7,10,17H,8-9,11H2,1H3,(H,21,23)
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| Chemical Name |
3,4-dichloro-N-[(2-methyl-3,4-dihydro-1H-isoquinolin-1-yl)methyl]benzamide
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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 |
| 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: 250 mg/mL (715.82 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.96 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 20.8 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: ≥ 2.08 mg/mL (5.96 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 20.8 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: ≥ 2.08 mg/mL (5.96 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8633 mL | 14.3164 mL | 28.6328 mL | |
| 5 mM | 0.5727 mL | 2.8633 mL | 5.7266 mL | |
| 10 mM | 0.2863 mL | 1.4316 mL | 2.8633 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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