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| 1mg |
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| Targets |
Neuropeptide FF receptors, specifically NPFF1 (also known as GPR147 or OT7T022) and NPFF2 (also known as GPR74 or HLWAR77). NPFF acts as an endogenous ligand for these G-protein-coupled receptors. The compound modulates pain perception by opposing the effects of opioid peptides. It also regulates cardiovascular function, neuroendocrine secretion, and gastrointestinal motility. NPFF receptors are potential targets for the development of analgesics and other therapeutic agents.
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| ln Vitro |
NPFF demonstrates a wide range of biological activities. It modulates pain perception by opposing the analgesic effects of opioids, acting as an anti-opioid peptide. The compound also regulates cardiovascular function by modulating blood pressure and heart rate. It inhibits the release of various hormones, including growth hormone and prolactin. NPFF also modulates gastrointestinal motility and feeding behavior. The compound's effects are mediated through its binding to NPFF1 and NPFF2 receptors.
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| ln Vivo |
NPFF has been studied in various in vivo models. In rodents, central or peripheral administration of NPFF modulates pain perception, cardiovascular function, and neuroendocrine secretion. The compound has been shown to reverse opioid-induced analgesia and to modulate opioid tolerance and dependence. NPFF also affects feeding behavior, reducing food intake in animal models. Its effects are dose-dependent and mediated through NPFF1 and NPFF2 receptors.
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| Enzyme Assay |
The in vitro receptor binding assay for NPFF typically involves measuring its binding affinity to NPFF1 and NPFF2 receptors using radioligand binding techniques. Membranes from cells expressing the recombinant receptors are incubated with a radiolabeled NPFF ligand and varying concentrations of the test compound. The binding affinity (Ki or IC50) is determined from the competition binding curves. Functional assays such as GTPγS binding or cAMP inhibition assays are also performed.
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| Cell Assay |
The in vitro cellular assay for NPFF typically involves the use of cells expressing NPFF1 or NPFF2 receptors. Cells are treated with NPFF or related peptides, and downstream signaling pathways (e.g., intracellular calcium mobilization, cAMP levels, or MAPK activation) are measured. The compound's ability to activate or inhibit receptor-mediated signaling is assessed. The EC50 or IC50 value is determined from the dose-response curve.
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| Animal Protocol |
In vivo animal studies for NPFF typically involve the administration of the peptide to rodents via intracerebroventricular (ICV), intrathecal (IT), or peripheral routes. Pain modulation is assessed using standard pain tests such as the tail-flick test or hot plate test. Cardiovascular function is monitored by measuring blood pressure and heart rate. Neuroendocrine effects are assessed by measuring hormone levels in blood. The compound's effects on opioid tolerance and dependence are also evaluated.
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| ADME/Pharmacokinetics |
NPFF is a neuropeptide with a molecular weight of approximately 883.0 g/mol and a molecular formula of C43H58N10O10. It is a peptide with limited oral bioavailability and is typically administered via injection. The compound is rapidly metabolized by peptidases in vivo and has a short half-life. Stable analogs of NPFF have been developed for research purposes to improve metabolic stability and bioavailability.
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| Toxicity/Toxicokinetics |
NPFF is a naturally occurring peptide and is generally well tolerated at physiological concentrations. However, the compound is intended for research use only and should be handled with appropriate laboratory safety precautions. Standard safety assessments would be required before any clinical application. Researchers should consult the safety data sheet for detailed handling information.
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| References | |
| Additional Infomation |
See also: ...View more...
NPFF is an endogenous neuropeptide that belongs to the RFamide peptide family. It is involved in the regulation of pain modulation, opioid tolerance, cardiovascular function, and neuroendocrine regulation. The compound exists in two main isoforms: NPFF-1 (FLFQPQRFamide) and NPFF-2 (SLAAPQRFamide). NPFF acts as an anti-opioid peptide and modulates pain perception by opposing the effects of opioids. It has not yet entered clinical trials and is strictly for preclinical research purposes. |
| Molecular Formula |
C54H76N14O10
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|---|---|
| Molecular Weight |
1081.26904
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| Exact Mass |
1080.59
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| CAS # |
99566-27-5
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| PubChem CID |
9854861
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| Appearance |
White to off-white solid powder
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| Density |
1.38 g/cm3
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| Index of Refraction |
1.656
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| LogP |
4.542
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| Hydrogen Bond Donor Count |
12
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
32
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| Heavy Atom Count |
78
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| Complexity |
2050
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| Defined Atom Stereocenter Count |
8
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| SMILES |
CC(C)C[C@@H](C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](CCC(=O)N)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC3=CC=CC=C3)C(=O)N)NC(=O)[C@H](CC4=CC=CC=C4)N
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| InChi Key |
HWYCFZUSOBOBIN-AQJXLSMYSA-N
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| InChi Code |
InChI=1S/C54H76N14O10/c1-32(2)28-41(66-47(72)36(55)29-33-14-6-3-7-15-33)50(75)67-42(31-35-18-10-5-11-19-35)51(76)64-39(23-25-45(57)70)53(78)68-27-13-21-43(68)52(77)63-38(22-24-44(56)69)49(74)62-37(20-12-26-61-54(59)60)48(73)65-40(46(58)71)30-34-16-8-4-9-17-34/h3-11,14-19,32,36-43H,12-13,20-31,55H2,1-2H3,(H2,56,69)(H2,57,70)(H2,58,71)(H,62,74)(H,63,77)(H,64,76)(H,65,73)(H,66,72)(H,67,75)(H4,59,60,61)/t36-,37-,38-,39-,40-,41-,42-,43-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S)-1-[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]-5-oxopentanoyl]pyrrolidine-2-carbonyl]amino]-N-[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]pentanediamide
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 (~92.48 mM)
H2O : ~50 mg/mL (~46.24 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.31 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 (2.31 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 (2.31 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 | 0.9248 mL | 4.6242 mL | 9.2484 mL | |
| 5 mM | 0.1850 mL | 0.9248 mL | 1.8497 mL | |
| 10 mM | 0.0925 mL | 0.4624 mL | 0.9248 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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