![[Met5]-Enkephalin, amide TFA (5-Methionine-enkephalin amide TFA)](/upload/1124/V69881.png)
| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
δ Opioid Receptor/DOR
delta opioid receptor (DOR) and putative zeta (zeta) opioid receptor. [Met5]-Enkephalin, amide TFA is an opioid receptor agonist, binding to and activating delta and zeta opioid receptors. Activation of these receptors leads to G-protein-mediated inhibition of adenylate cyclase and modulation of ion channels. |
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| ln Vitro |
[Met5]-Enkephalin dramatically lowers the total number of glial cells in culture at concentrations of 0.1 nM, 10 nM, and 1 μM [1]. Cats' pelvic nerve-induced distal colon contractions are inhibited by [Met5]-Enkephalin, amide, which works through delta-opioid receptors. [Met5]-enkephalin has an IC50 value of 2.2 nM and inhibits pelvic nerve-evoked contractions in a concentration-dependent and reversible manner. At a high dosage (3 nM), [Met5]enkephalin strongly suppresses neurogenic contractions, but exogenous acetylcholine-induced contractions are unaffected [2].
Specific in vitro activity data such as IC50 or Ki values for receptor binding are not reported. As an enkephalin analogue, it is expected to exhibit nM-range affinity for delta and zeta opioid receptors. Cats‘ pelvic nerve-induced distal colon contractions are inhibited by [Met5]-Enkephalin, amide, which works through delta-opioid receptors, confirming its functional agonist activity in a bioassay context. |
| ln Vivo |
No specific in vivo activity data are reported for this compound in the literature. As an enkephalin analogue, it would be expected to produce opioid-mediated analgesic effects in animal models of pain (e.g., tail-flick, hot-plate, or writhing tests) when administered centrally, but such studies have not been published for this specific amide derivative. It is used primarily as an in vitro pharmacological tool.
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| Enzyme Assay |
Cell-free radioligand binding assays for delta and zeta opioid receptors are performed using brain membrane preparations (e.g., rat or mouse whole brain minus cerebellum). Membranes are incubated with the appropriate radioligand (e.g., [3H]-[D-Pen2,D-Pen5]enkephalin (DPDPE) for delta receptors or [3H]-naloxone for total opioid receptors) and increasing concentrations of [Met5]-Enkephalin, amide TFA (0.01-10,000 nM) in 50 mM Tris-HCl (pH 7.4) containing 1 mM EDTA and 0.1% BSA for 60 min at 25degC. Bound radioactivity is separated by GF/B filtration. IC50 values are calculated by nonlinear regression.
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| Cell Assay |
Cell-based assays can be performed using CHO cells stably expressing delta opioid receptors. Cells are loaded with a fluorescent calcium indicator or a cAMP detection kit. [Met5]-Enkephalin, amide TFA is added at increasing concentrations (0.1-1000 nM), and changes in intracellular calcium or cAMP levels are measured. Functional activation of the delta receptor is assessed by inhibition of forskolin-stimulated cAMP accumulation (HTRF assay) or by calcium mobilization (FLIPR). EC50 values are determined from dose-response curves. For colon contraction bioassays, cat distal colon segments are mounted in organ baths and electrically field-stimulated; [Met5]-Enkephalin, amide TFA (0.1-100 nM) is added to inhibit nerve-evoked contractions via delta receptors.
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| Animal Protocol |
No in vivo animal protocols are published for this specific compound. For general enkephalin analog studies, the compound would be administered intracerebroventricularly (i.c.v.) in rodents (1-100 ug/mouse) after being dissolved in sterile artificial CSF. Analgesia would be assessed using hot plate or tail-flick tests at 5-30 min post-injection. However, these studies have not been specifically reported for [Met5]-Enkephalin, amide TFA.
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| ADME/Pharmacokinetics |
No specific pharmacokinetic data are reported for [Met5]-Enkephalin, amide TFA. As a peptide, it is not orally bioavailable and has a very short plasma half-life (minutes) due to rapid degradation by peptidases. The amidation of the C-terminus may confer some resistance to carboxypeptidase degradation compared to the free acid form. The molecular weight is 686.70 (C29H37F3N6O8S). The peptide sequence is Tyr-Gly-Gly-Phe-Met-NH2. Solubility: Water 90 mg/mL. Storage: -20degC, dry, sealed, away from moisture.
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| Toxicity/Toxicokinetics |
No toxicity data are reported for this compound. As a research peptide, standard safety assessments have not been conducted. At the concentrations used in in vitro assays (nM to uM), no overt cytotoxicity has been observed. The TFA salt form contains trifluoroacetate, which may be toxic at high concentrations (>1% in formulations); however, at experimental concentrations, it is generally considered biocompatible. The compound is for research use only.
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| References | |
| Additional Infomation |
Other information: [Met5]-Enkephalin, amide TFA (CAS 2918768-28-0) is a research-grade peptide, not FDA-approved. Purity ≥98% . The compound is also known as 5-Methionine-enkephalin amide TFA. It is a valuable research tool for studying delta and zeta opioid receptor pharmacology in vitro, including receptor binding, signaling, and colon motility assays. It is not intended for human use.
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| Exact Mass |
686.235
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| CAS # |
2918768-28-0
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| Related CAS # |
[Met5]-Enkephalin, amide;60117-17-1
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| PubChem CID |
138911447
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
47
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| Complexity |
931
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CSCC[C@@H](C(=O)N)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)CNC(=O)CNC(=O)[C@H](CC2=CC=C(C=C2)O)N.C(=O)(C(F)(F)F)O
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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) |
H2O: 100 mg/mL (145.62 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (72.81 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
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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