Reagentia en instrumenten voor immunologie, celbiologie en moleculaire biologie.

Nociceptin [170713-75-4]

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Referentie HY-P0183-1mg

Formaat : 1mg

Merk : MedChemExpress

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Description

Nociceptin, a heptadecapeptide, is the endogenous ligand of the nociceptin receptor, acting as a potent anti-analgesic.

Cellular Effect

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	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]
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]
COS-7	EC₅₀	1.1 nM Compound: [Arg(14),Lys(15)]Nociceptin	Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding	[PMID: 19879767]
COS-7	EC₅₀	1.1 nM Compound: [Arg(14),Lys(15)]Nociceptin	Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding	[PMID: 19879767]
COS-7	EC₅₀	1.2 nM Compound: [Arg(14),Lys(15)]Nociceptin	Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding	[PMID: 19879767]
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	EC₅₀	13 nM Compound: nociceptin	Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding	[PMID: 19879767]
COS-7	EC₅₀	13 nM Compound: nociceptin	Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding	[PMID: 19879767]
COS-7	EC₅₀	21 nM Compound: nociceptin	Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding	[PMID: 19879767]
COS-7	EC₅₀	25 nM Compound: nociceptin	Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding	[PMID: 19879767]
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	EC₅₀	5.6 nM Compound: [Arg(14),Lys(15)]Nociceptin	Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding	[PMID: 19879767]
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	0.21 nM Compound: [Arg(14),Lys(15)]Nociceptin	Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay	[PMID: 19879767]
COS-7	IC₅₀	0.22 nM Compound: [Arg(14),Lys(15)]Nociceptin	Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay	[PMID: 19879767]
COS-7	IC₅₀	0.22 nM Compound: [Arg(14),Lys(15)]Nociceptin	Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay	[PMID: 19879767]
COS-7	IC₅₀	0.46 nM Compound: [Arg(14),Lys(15)]Nociceptin	Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay	[PMID: 19879767]
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	0.54 nM Compound: [Arg(14),Lys(15)]Nociceptin	Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay	[PMID: 19879767]
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	IC₅₀	0.65 nM Compound: nociceptin	Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay	[PMID: 19879767]
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	0.72 nM Compound: nociceptin	Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay	[PMID: 19879767]
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	0.8 nM Compound: nociceptin	Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay	[PMID: 19879767]
COS-7	IC₅₀	0.91 nM Compound: nociceptin	Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay	[PMID: 19879767]
COS-7	IC₅₀	1.02 nM Compound: nociceptin	Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay	[PMID: 19879767]
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	0.23 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]
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]

In Vitro

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.

Solvant et solubilité

In Vitro:

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	0.5528 mL	2.7639 mL	5.5278 mL
5 mM	0.1106 mL	0.5528 mL	1.1056 mL
10 mM	0.0553 mL	0.2764 mL	0.5528 mL

View the 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.

* 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.

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (1.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.

Protocol 1

Add each solvent one by one: PBS
Solubility: 50 mg/mL (27.64 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Pureté et documentation

Purity: 98.09%

Fiche technique (274 KB) SDS (252 KB)

COA (245 KB) RP-HPLC (206 KB) LCMS (99 KB) Elemental Analysis Report (103 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Bedini A, et al. Nociceptin/orphanin FQ antagonizes lipopolysaccharide-stimulated proliferation, migration and inflammatory signaling in human glioblastoma U87 cells. Biochem Pharmacol. 2017 Sep 15;140:89-104. [Content Brief]

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