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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
NOP Receptor/ORL1
Nociceptin (1-13), amide TFA specifically and potently targets the ORL1 receptor (Opioid Receptor-Like 1), a class A G-protein coupled receptor (GPCR). Despite its sequence and structural similarity to classical opioid receptors (mu, delta, kappa), ORL1 has a distinct pharmacology and does not bind traditional opioid ligands with high affinity. Activation of ORL1 primarily leads to its coupling with Gi/o proteins, resulting in the inhibition of adenylyl cyclase and a subsequent decrease in intracellular cAMP levels. It also opens inwardly rectifying potassium channels (GIRKs) and closes voltage-gated calcium channels (VGCCs), which can hyperpolarize neurons and inhibit neurotransmitter release. This mechanism is fundamental to its role in modulating pain signals, stress responses, and other neurological functions. This agonist is highly potent with a binding affinity Ki of 0.75 nM for rat forebrain membranes. |
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| ln Vitro |
The in vitro activity of Nociceptin (1-13), amide TFA is characterized by its potent agonism at the ORL1 receptor. Its functional potency is demonstrated by its ability to inhibit electrically evoked contractions in the isolated mouse vas deferens (MVD) tissue, where it exhibits a pEC50 of 7.9 (EC50 = ~12.6 nM). This assay is a classical bioassay for measuring opioid-like activity. Additionally, the binding affinity of the compound has been determined by radioligand binding assays in rat forebrain membranes, yielding a very high affinity Ki value of 0.75 nM. This high affinity and potent functional activity make it a standard pharmacological tool for exploring ORL1 biology.
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| ln Vivo |
No specific in vivo data is available for this truncated (1-13) amide fragment in the search results. However, its effects are expected to mirror those of the parent full-length nociceptin/orphanin FQ peptide. The full-length peptide is known to be widely involved in various physiological and pathological processes in animal models. For instance, intracerebroventricular (i.c.v.) administration of nociceptin induces hyperalgesia (increased sensitivity to pain) in some paradigms, in contrast to the analgesic effects of classical opioids. It also plays a role in stress responses and anxiety, as well as in regulating locomotor activity. In reward pathways, nociceptin can oppose the effects of drugs of abuse. As a potent agonist, this fragment is expected to reproduce these core in vivo actions of the nociceptin system. The TFA salt form enhances its solubility for such central administrations.
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| Enzyme Assay |
A cell-free membrane binding assay is used to assess the affinity of the peptide for the ORL1 receptor. The protocol involves isolating a membrane fraction from rat forebrain or from cells expressing recombinant human ORL1 receptors. For a competition binding assay, the membranes (10-20 ug protein/well) are incubated with a fixed, low concentration of a radiolabeled tracer, such as [3H]-nociceptin (0.1-1 nM), in a 96-well plate at 25degC for 60 minutes. Serial dilutions of unlabeled Nociceptin (1-13), amide TFA (ranging from 0.1 pM to 10 uM) are added to compete with the tracer. Non-specific binding is determined in the presence of a high concentration of unlabeled nociceptin (1-10 uM). The reaction is terminated by rapid filtration through GF/B glass fiber filters, followed by several washes with ice-cold 50 mM Tris-HCl buffer (pH 7.4). The filters are dried, and the bound radioactivity is counted. The Ki value (0.75 nM) is calculated from the IC50 of the competition curve.
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| Cell Assay |
The mouse vas deferens (MVD) assay is a functional in vitro bioassay. Male mice (e.g., CD-1 strain, 25-35 g) are sacrificed by cervical dislocation, and both vasa deferentia are removed and placed in oxygenated (95% O2, 5% CO2) Krebs-Henseleit buffer (pH 7.4). Each vas deferens is mounted under 0.5 g tension in a 5-10 mL organ bath containing the buffer maintained at 37degC. The tissues are allowed to equilibrate for 30 minutes with regular buffer changes. Field stimulation is applied via platinum ring electrodes using a stimulator delivering square-wave pulses (0.1 Hz, 1 ms duration, suprathreshold voltage). Once the baseline twitch contractions are stable, cumulative concentrations of Nociceptin (1-13), amide TFA (0.1 nM to 10 uM) are added to the bath. Each concentration is allowed to act for 2-5 minutes before the next addition. The extent of inhibition of the electrically evoked twitch contractions is recorded. The pEC50 value (7.9) is determined as the negative logarithm of the concentration producing 50% of the maximal inhibition.
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| Animal Protocol |
The in vivo activity of the nociceptin system is typically studied in rodent models of pain, stress, and addiction. A common experimental protocol involves the use of adult male C57BL/6 or Swiss-Webster mice. The compound (Nociceptin (1-13), amide TFA) is dissolved in artificial cerebrospinal fluid (aCSF) or saline. It is administered by the intracerebroventricular (i.c.v.) route (e.g., 1-10 microg in a 2-5 microL volume per mouse) to bypass the blood-brain barrier. The injection is made directly into the lateral ventricle using a stereotaxic frame or a free-hand method. After injection, animals are subjected to behavioral testing. For pain studies, a tail-flick test can be performed by immersing the tail tip in warm water (52degC) and recording the latency to a reflexive flick. A hot plate test (55degC) is also used, measuring the time to paw licking or jumping. For stress or anxiety studies, the elevated plus maze (EPM) or open field test is used. These experiments typically involve recording behavior for 5-10 minutes post-administration to assess the central effects of ORL1 activation.
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| ADME/Pharmacokinetics |
Nociceptin (1-13), amide TFA (MW: 1495.61) should be stored as a lyophilized powder at -20degC, protected from moisture and light. Under these conditions, it is stable for up to 3 years. For in vitro assays, a stock solution can be prepared by dissolving the powder in DMSO to a concentration of 100 mg/mL or more. For a working solution, it is then diluted in the appropriate aqueous buffer. The TFA salt is used to enhance its water solubility. In vivo, the compound is typically formulated in a solution of 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline to create a clear solution for injection. Due to its peptide nature, it is expected to have a short plasma half-life (minutes), making it most suitable for acute central administration.
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| Toxicity/Toxicokinetics |
This product is for research use only and is not for human therapeutic applications. The potential toxicity of this peptide is not well-documented in the search results. However, standard laboratory safety practices should be followed, including the use of lab coats, gloves, and safety glasses when handling the powder or solutions. The trifluoroacetic acid (TFA) counterion can be toxic to cells if present in high concentrations. No known acute toxicity has been reported in animal studies at the low, acute doses typically used in research. The ORL1 receptor system is known to be involved in pain modulation, and its activation might produce on-target effects in vivo if administered systemically.
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| References | |
| Additional Infomation |
This product is a 13-amino acid peptide sequence (FGGFTGARKSARK-NH2) derived from the longer nociceptin peptide. It has a molecular weight of 1495.61 g/mol. Nociceptin is also known as orphanin FQ, and its discovery in the mid-1990s led to the identification of the ORL1 receptor as a new member of the opioid receptor family. Unlike classic opioids that are primarily analgesic, the nociceptin system has a complex and often opposing role in pain modulation, depending on the site of action. It is an important target for drug development for conditions like anxiety, depression, addiction, and chronic pain. The TFA salt form is a common synthetic counterion used to improve the physicochemical properties of peptides for research applications.
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| Molecular Formula |
C63H101F3N22O17
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| Molecular Weight |
1495.61
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| Related CAS # |
Nociceptin (1-13), amide;178064-02-3
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| Appearance |
Solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :≥ 100 mg/mL (~66.86 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.67 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (1.67 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (1.67 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.6686 mL | 3.3431 mL | 6.6862 mL | |
| 5 mM | 0.1337 mL | 0.6686 mL | 1.3372 mL | |
| 10 mM | 0.0669 mL | 0.3343 mL | 0.6686 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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