BPR1M97 |
Catalog No.GC38741
One-Click Copy Product Info
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BPR1M97 is a novel, dual-activity agonist of the mu-opioid receptor (MOP) and the nociceptin/orphanin FQ peptide (NOP) receptor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2059904-66-2
Sample solution is provided at 25 µL, 10mM.
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BPR1M97 is a novel, dual-activity agonist of the mu-opioid receptor (MOP) and the nociceptin/orphanin FQ peptide (NOP) receptor. BPR1M97 produces potent analgesic effects by simultaneously activating both MOP and NOP receptors, while exhibiting fewer adverse reactions compared to morphine. BPR1M97 is used for pain management and related research[1].
In vitro, cells expressing the human mu-opioid receptor (MOP) and/or the nociceptin/orphanin FQ peptide (NOP) receptor (e.g., HEK-MOP, CHO-K1-NOP, U2OS-MOP) were treated with BPR1M97 (0.6nM – 1.9µM) for 0.5 to 1.5 hours. BPR1M97 significantly inhibited intracellular cAMP levels, activated GIRK channels, and induced β-arrestin-2 recruitment and receptor internalization[1].
In vivo, normal ICR mice or mice with neuropathic pain models were subcutaneously administered a single dose of BPR1M97 (0.2-9mg/kg). BPR1M97 produced a dose-dependent and potent analgesic effect. At high doses, the respiratory depression it induced was significantly less severe than that caused by equi-analgesic doses of morphine[1].
References:
[1] Chao PK, Chang HF, Chang WT, et al. BPR1M97, a dual mu opioid receptor/nociceptin-orphanin FQ peptide receptor agonist, produces potent antinociceptive effects with safer properties than morphine. Neuropharmacology. 2020 Apr;166:107678.
| Cell experiment [1]: | |
Cell lines | HEK-MOP cells (human embryonic kidney 293 cells constitutively expressing the human mu opioid receptor), CHO-K1-NOP cells (Chinese hamster ovary cells expressing the human nociceptin-orphanin FQ peptide receptor), U2OS-MOP cells (human osteosarcoma cells expressing human MOP), and myc-MOP-expressing mouse pituitary AtT-20 cells |
Preparation Method | HEK-MOP cells were cultured in high-glucose DMEM supplemented with 10% fetal bovine serum (FBS). CHO-K1-NOP cells were cultured in F12 medium containing 10% FBS. U2OS-MOP cells were cultured in McCoy's 5A medium with 10% FBS. AtT-20 cells were cultured in DMEM with 10% FBS. Cells were treated with BPR1M97 at concentrations ranging from 0.6nM to 1.9µM. Incubation times varied by assay: 30 minutes for the cAMP assay, 1.5 hours for the β-arrestin-2 recruitment and receptor internalization assays, and 0.5 hours of pre-treatment with dye followed by real-time monitoring for the membrane potential assay. |
Reaction Conditions | 0.6nM–1.9μM; 0.5-1.5h. |
Applications | In MOP-expressing cells, BPR1M97 acted as a full agonist, significantly inhibiting cAMP production, activating GIRK channels, recruiting β-arrestin-2, and inducing receptor internalization. In NOP-expressing cells, BPR1M97 acted as a G protein-biased full agonist, inhibiting cAMP production but failing to recruit β-arrestin-2. |
| Animal experiment [1]: | |
Animal models | ICR mice, formalin-induced inflammatory pain model in ICR mice, and chronic constriction injury (CCI)-induced neuropathic pain model in ICR mice. |
Preparation Method | Mice were subcutaneously (s.c.) administered a single dose of BPR1M97. For thermal and mechanical nociception tests, behavioral responses were recorded at specified time points post-injection. For tolerance and dependence studies, mice received twice-daily injections for 5 days. |
Dosage form | 0.2-9mg/kg; s.c.; Single or twice-daily injections for 5 days |
Applications | BPR1M97 produced potent, dose-dependent antinociception in acute thermal, acute mechanical with efficacy comparable or superior to morphine. BPR1M97 caused significantly less respiratory depression, cardiovascular inhibition. BPR1M97 also induced conditioned place preference (reward effect) but with lower hyperlocomotor activity. |
References: | |
| Cas No. | 2059904-66-2 | SDF | |
| Canonical SMILES | O=C(NCC1N(C)CCC2=C1C=CC=C2)C3=CC=C(Cl)C(Cl)=C3 | ||
| Formula | C18H18Cl2N2O | M.Wt | 349.25 |
| Solubility | DMSO: 250 mg/mL (715.82 mM) | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8633 mL | 14.3164 mL | 28.6328 mL |
| 5 mM | 572.7 μL | 2.8633 mL | 5.7266 mL |
| 10 mM | 286.3 μL | 1.4316 mL | 2.8633 mL |
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g
μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)