Nociceptin
Based on 5 publication(s) in Google Scholar
Nociceptin, a heptadecapeptide, is the endogenous ligand of the nociceptin receptor, acting as a potent anti-analgesic.
For research use only. We do not sell to patients.
- Purity: 98.09%
- CAS No.: 170713-75-4
- Formula: C79H129N27O22
- Molecular Weight:1809.04
-
Storage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocol
- Purity & Documentation
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Nociceptin
MoreAll Opioid Receptor Isoforms
More
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
0.08 nM
Compound: Nociceptin
|
Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data
Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data
|
[PMID: 12372523] |
| CHO | EC50 |
78.5 nM
Compound: NOP, Orphanin FQ
|
Partial agonist activity at human KOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
Partial agonist activity at human KOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
|
[PMID: 21866885] |
| CHO | EC50 |
8.1 nM
Compound: NOP, Orphanin FQ
|
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
|
[PMID: 21866885] |
| CHO | EC50 |
3.6 nM
Compound: orphanin FQ, N/OFQ
|
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
|
[PMID: 24657054] |
| COS-7 | EC50 |
3.91 nM
Compound: nociceptin
|
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
|
[PMID: 18068993] |
| COS-7 | IC50 |
0.6 nM
Compound: nociceptin
|
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
|
[PMID: 18068993] |
| COS-7 | EC50 |
13 nM
Compound: Nociceptin, Noc
|
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
|
[PMID: 18818087] |
| COS-7 | IC50 |
0.73 nM
Compound: Nociceptin, Noc
|
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
|
[PMID: 18818087] |
| COS-7 | IC50 |
0.52 nM
Compound: nociceptin
|
Displacement of [3H]nociceptin from rat Galpha-fused ORL1 receptor expressed in african green monkey COS7 cells
Displacement of [3H]nociceptin from rat Galpha-fused ORL1 receptor expressed in african green monkey COS7 cells
|
[PMID: 22061823] |
| COS-7 | IC50 |
0.084 nM
Compound: Nociceptin
|
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
|
[PMID: 25284251] |
| COS-7 | IC50 |
0.65 nM
Compound: Nociceptin
|
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
|
[PMID: 25284251] |
| COS-7 | IC50 |
1.83 nM
Compound: Nociceptin
|
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
|
[PMID: 25284251] |
| HEK293 | EC50 |
0.45 nM
Compound: 1
|
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
|
[PMID: 12431054] |
| HEK293 | EC50 |
1.5 nM
Compound: N/OFQ
|
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
|
[PMID: 19125610] |
| HEK293 | EC50 |
1.5 nM
Compound: N/OFQ
|
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
|
[PMID: 20875743] |
| HEK293 | IC50 |
1.3 nM
Compound: Nociceptin
|
Displacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cells
Displacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cells
|
[PMID: 26988801] |
| HEK293 | EC50 |
0.23 nM
Compound: nociceptin; orphanin FQ
|
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
|
[PMID: 27035422] |
Nociceptin (1 μg/mL) significantly prevents LPS (10 ng/mL)-stimulated cell migration whereas it is ineffective when added alone. Nociceptin (1 nM-10 μM) elicits a concentration-dependent blockade of LPS-mediated cell migration, with a maximal effect at 1 and 10 μM. Nociceptin counteracts LPS-induced elevation of IL-1β mRNA levels. Nociceptin (1 μM) and NNC 55-0396 induce apoptotic cell death in U87 cells. Nociceptin (1 μM) counteracts LPS-induced [Ca2+]i increase in U87 cells via β-arrestin 2. Nociceptin counteracts the LPS-induced phosphorylation of PKC and ERK in U87 cells. Nociceptin inhibits the LPS-mediated transcriptional activation of NF-kB and AP-1 reporter genes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 170713-75-4
-
Appearance Solid
-
Molecular Weight 1809.04
-
Formula C79H129N27O22
-
Color White to off-white
-
Synonyms
Orphanin FQ
-
Sequence
Phe-Gly-Gly-Phe-Thr-Gly-Ala-Arg-Lys-Ser-Ala-Arg-Lys-Leu-Ala-Asn-Gln
-
Sequence Shortening
FGGFTGARKSARKLANQ
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (5)
-
Journal Impact Factor
-
Most Recent
-
Neurotherapeutics
LY2940094, an NOPR antagonist, promotes oligodendrocyte generation and myelin recovery in an NOPR independent manner. [Abstract]2024 Sep;21(5):e00424. PMID: 39004556 -
Neuropeptides
2026 Feb:115:102570. PMID: 41349199 -
-
-
bioRxiv
Development of a genetically encoded sensor for probing endogenous nociceptin opioid peptide release. [Abstract]2024 May 22:2023.05.26.542102. PMID: 37292957
Solvent & Solubility
DMSO : 50 mg/mL (27.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 50 mg/mL (27.64 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (1.38 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (1.38 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (27.64 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocol
Cell proliferation assay is carried out in the assay. U87 cells are plated on 12-well plate and treated for 24 h maintained in cell culture medium containing 10% fetal bovine serum. Five hours before the end of the treatments, [methyl-3H] Thymidine (50 nM final concentration) is added to serum-free cell culture medium and the plate is incubated at 37°C. Thereafter, medium is removed and cells are washed twice with PBS. 200 μL of PBS is added to each well, the cells are scraped off and centrifuged at 13,000g for 3 min at 4°C; supernatants are then discarded, pellets resuspended in 500 μL of cold trichloroacetic acid (10% w/v), incubated on ice for 20 min and centrifuged at 13,000g for 3 min at 4°C. The obtained supernatant is then discarded, pellet suspended in 500 μL of cold methanol and centrifuged at 3 min for 13,000g at 4°C. After that, the pellet is suspended in 200 μL of NaOH 1 N and heated at 55°C for 10 min. Samples are then neutralized with 200 μL of HCl 1 N and 350 μL of the labeled DNA incubated in counting vials with 4 mL of Filter Count scintillation liquid. Vials are vortexed and incubated overnight at room temperature and the radioactivity is determined by liquid scintillation spectrometry.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
-
Data Sheet (274 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 0.5528 mL | 2.7639 mL | 5.5278 mL | 13.8195 mL |
| 5 mM | 0.1106 mL | 0.5528 mL | 1.1056 mL | 2.7639 mL | |
| 10 mM | 0.0553 mL | 0.2764 mL | 0.5528 mL | 1.3819 mL | |
| 15 mM | 0.0369 mL | 0.1843 mL | 0.3685 mL | 0.9213 mL | |
| 20 mM | 0.0276 mL | 0.1382 mL | 0.2764 mL | 0.6910 mL | |
| 25 mM | 0.0221 mL | 0.1106 mL | 0.2211 mL | 0.5528 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Nociceptin Related Classifications
HY-P0183 Related Classifications
Powered by Bioz