Nociceptin (Synonyms: 孤菲肽; Orphanin FQ)

目录号: HY-P0183 纯度: 98.36%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Nociceptin 是一种十七肽，为 nociceptin 受体的内源性配体，具有缓解疼痛的作用。

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Custom Peptide Synthesis

Nociceptin Chemical Structure

CAS No. : 170713-75-4

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规格	价格	是否有货
1 mg	￥700	In-stock
5 mg	￥2800	In-stock
10 mg	￥5100	In-stock
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100 mg		询价

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MCE 顾客使用本产品发表的 2 篇科研文献

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查看所有亚型

μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

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

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
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	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 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	0.22 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	0.46 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	0.54 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	0.65 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	0.8 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]
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]
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	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]

体外研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

1809.04

Formula

C₇₉H₁₂₉N₂₇O₂₂

CAS 号

170713-75-4

性状

固体

颜色

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

中文名称

孤菲肽；痛敏肽；孤啡肽

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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)

溶解性数据

细胞实验：

DMSO 中的溶解度 : 50 mg/mL (27.64 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H₂O 中的溶解度 : ≥ 50 mg/mL (27.64 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	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

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

摩尔计算器
稀释计算器

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (1.38 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (1.38 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (1.38 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： PBS
Solubility: 50 mg/mL (27.64 mM); 澄清溶液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

计算结果

工作液所需浓度 : mg/mL

该产品水溶性佳，请具体参考实测水 / PBS / Saline 中的溶解度数据。

您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。

纯度 & 产品资料

纯度: 98.70%

选择批次：

Data Sheet (623 KB) SDS (252 KB)

COA (282 KB) RP-HPLC (206 KB) 元素分析报告 (206 KB)

产品使用指南 (1538 KB)

参考文献

[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]

Cell Assay ^[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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[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]

Cell Assay
^[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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

[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]

Nociceptin 相关分类

Neurological Disease

完整储备液配制表

可选溶剂	浓度溶剂体积质量	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

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Nociceptin170713-75-4Orphanin FQ孤菲肽痛敏肽孤啡肽Opioid ReceptorInhibitorinhibitorinhibit

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Nociceptin (Synonyms: 孤菲肽; Orphanin FQ)

Customer Review

MCE 顾客使用本产品发表的 2 篇科研文献

Nociceptin 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Opioid Receptor 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

Nociceptin 相关分类

完整储备液配制表

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Nociceptin (Synonyms: 孤菲肽; Orphanin FQ)

Customer Review

Nociceptin 相关抗体

MCE 顾客使用本产品发表的 2 篇科研文献

Nociceptin 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Opioid Receptor 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

Nociceptin 相关抗体:

摩尔计算器

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Nociceptin 相关分类

完整储备液配制表

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