1. GPCR/G Protein Neuronal Signaling
  2. Opioid Receptor
  3. Nociceptin

ノシセプチン  (Synonyms: Nociceptin; Orphanin FQ)

製品番号: HY-P0183 純度: 98.09%
COA 取扱説明書 Technical Support

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

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カスタムペプチド

Nociceptin

ノシセプチン 構造式

CAS 番号 : 170713-75-4

容量 価格(税別) 在庫状況 数量
1 mg $92 在庫あり
5 mg $290 在庫あり
10 mg $470 在庫あり
25 mg $950 在庫あり
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100 mg   お問い合わせ  

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カスタマーレビュー

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products
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製品説明

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 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
1.1 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
1.2 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 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
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
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 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
0.65 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
0.72 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]
体外実験

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.

臨床実験
分子量

1809.04

分子式

C79H129N27O22

CAS 番号
Appearance

Solid

Color

White to off-white

Sequence

Phe-Gly-Gly-Phe-Thr-Gly-Ala-Arg-Lys-Ser-Ala-Arg-Lys-Leu-Ala-Asn-Gln

Sequence Shortening

FGGFTGARKSARKLANQ

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Sealed storage, away from moisture
Powder -80°C 2 years
  -20°C 1 year
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

C1

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体積 (開始)

V1

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体内:

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.

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:

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g

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(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).
純度とドキュメンテーション
参考文献
細胞実験
[1]

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) はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献

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.

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  • Molarity Calculator

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
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製品名:
Nociceptin
製品番号:
HY-P0183
数量:
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