| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
FMRFamide receptors (GPCRs) and amiloride-sensitive sodium channels.
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| ln Vitro |
In vitro, FMRF interacts with specific G-protein coupled receptors, influencing signal transduction pathways in the nervous system. The neuropeptide stimulates enzyme activity 7- to 8-fold (EC₅0 = 1 microM) via pharmacologically distinct receptors. FMRF induces a fast excitatory depolarizing response due to direct activation of amiloride-sensitive sodium channels. The peptide is involved in regulating cardiac function, feeding behavior, and reproductive activities.
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| ln Vivo |
In vivo, FMRF has been used as a research tool to study neurochemical interactions and their impact on behavior and physiology in animal models. It influences various physiological processes such as cardiac function, feeding behavior, and reproductive activities. The peptide is primarily used in neuropharmacological studies to understand the role of RFamide peptides in nervous system function.
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| Enzyme Assay |
Receptor binding assays are performed using membrane preparations from tissues or cells expressing FMRFamide receptors. Membranes are incubated with radiolabeled [¹2⁵I]-FMRF or [3H]-FMRF and varying concentrations of unlabeled FMRF (1 nM-100 microM) in binding buffer (50 mM Tris-HCl, pH 7.4, containing 0.5% BSA and protease inhibitors) at room temperature for 60-120 minutes. Non-specific binding is determined in the presence of 1-10 microM unlabeled FMRF. Bound and free ligand are separated by rapid filtration through GF/B or GF/C filters. Radioactivity is counted and binding parameters are calculated. For sodium channel activation studies, patch-clamp electrophysiology is performed on cells expressing amiloride-sensitive sodium channels to measure FMRF-induced currents.
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| Cell Assay |
Functional assays are performed in cells expressing FMRFamide receptors (e.g., HEK-293 cells) or in primary neuronal cultures. Cells are seeded in 96-well plates and treated with FMRF at concentrations ranging from 0.01 nM to 100 microM. Receptor activation is assessed by measuring calcium mobilization using fluorescent calcium indicators (e.g., Fluo-4), cAMP accumulation assays, or GTPgammaS binding assays. For enzyme activity studies, the peptide is added to cell lysates or tissue homogenates and enzyme activity is measured using appropriate substrates. EC₅0 values are calculated from dose-response curves.
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| Animal Protocol |
In vivo studies are performed in invertebrate models (e.g., mollusks) or rodent models depending on the experimental question. FMRF is administered via intracerebroventricular (ICV) or intravenous injection at doses ranging from 0.1-10 nmol. Behavioral endpoints such as feeding behavior, locomotor activity, or cardiovascular parameters are measured at multiple time points post-administration. Tissue samples may be collected for receptor occupancy studies or neurochemical analysis. The specificity of observed effects is confirmed using FMRF receptor antagonists or by comparing with related RFamide peptides.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of FMRF (MW 599.74, C2₉H41N₇O₅S) are characteristic of small peptides: rapid degradation by peptidases, short half-life in biological matrices, and poor oral bioavailability. The peptide is typically administered parenterally for research applications. It is soluble in DMSO (100 mg/mL) and other appropriate solvents. Stability is enhanced by storage as a lyophilized powder at -20degC.
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| Toxicity/Toxicokinetics |
No specific toxicity data are reported for FMRF. As a neuroactive peptide, it is expected to have effects on the nervous system at pharmacological doses. The compound is for research use only and not for human therapeutic use. Standard safety precautions for handling peptides should be observed.
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| Additional Infomation |
neuroactive peptide from a mollusc can induce a rapid excitatory depolarization response by directly activating amiloride-sensitive sodium channels. (Excerpt from Nature 1995; 378(6558): 730-3)
FMRF (Phe-Met-Arg-Phe) is a tetrapeptide consisting of four amino acid residues. It is a member of the RFamide peptide family and serves as a model compound for studying neuropeptide signaling. The peptide is used as a research tool to investigate FMRFamide receptor pharmacology, sodium channel modulation, and neuropeptide-receptor interactions. FMRF is not an approved therapeutic agent; it is exclusively a research compound. The peptide is available as a research-grade compound with purity >98% (HPLC) for laboratory use. |
| Molecular Formula |
C29H41N7O5S
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|---|---|
| Molecular Weight |
599.744745016098
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| Exact Mass |
599.289
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| CAS # |
74012-06-9
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| PubChem CID |
9916730
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| Appearance |
White to off-white solid powder
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| LogP |
4.766
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
42
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| Complexity |
890
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CSCC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)O)NC(=O)[C@H](CC2=CC=CC=C2)N
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| InChi Key |
QXYYONMTJKILDK-ZJZGAYNASA-N
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| InChi Code |
InChI=1S/C29H41N7O5S/c1-42-16-14-23(34-25(37)21(30)17-19-9-4-2-5-10-19)27(39)35-22(13-8-15-33-29(31)32)26(38)36-24(28(40)41)18-20-11-6-3-7-12-20/h2-7,9-12,21-24H,8,13-18,30H2,1H3,(H,34,37)(H,35,39)(H,36,38)(H,40,41)(H4,31,32,33)/t21-,22-,23-,24-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-phenylpropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-phenylpropanoic acid
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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 (~166.74 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.17 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 (4.17 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 (4.17 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 | 1.6674 mL | 8.3369 mL | 16.6739 mL | |
| 5 mM | 0.3335 mL | 1.6674 mL | 3.3348 mL | |
| 10 mM | 0.1667 mL | 0.8337 mL | 1.6674 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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