| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Leuphasyl targets delta opioid receptors, acting as an agonist. Delta opioid receptors are G protein-coupled receptors involved in the regulation of pain, mood, and reward. By activating these receptors, leuphasyl modulates signaling pathways that influence neurotransmitter release and muscle contraction. The compound inhibits the release of acetylcholine and inhibits muscle contraction. Its resistance to degradation makes it a long-acting tool for studying opioid receptor signaling.
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| ln Vitro |
In vitro, leuphasyl acts as a delta opioid agonist. It inhibits the release of acetylcholine and inhibits muscle contraction. Detailed IC₅₀ or EC₅₀ values for receptor activation are not extensively reported in the available literature. The compound's resistance to degradation suggests it may have prolonged activity in vitro. Its activity is confirmed through receptor binding and functional assays.
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| ln Vivo |
Detailed in vivo activity data for leuphasyl are not extensively reported in the available literature. As a delta opioid agonist, it is expected to have effects on pain, mood, and muscle function. However, specific in vivo efficacy data from animal studies are not provided in the available sources. Further studies are needed to confirm its therapeutic potential.
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| Enzyme Assay |
Non-cell-based receptor binding assays for leuphasyl typically involve radioligand binding studies using membrane preparations from cells expressing human delta opioid receptors. The receptor is incubated with a radiolabeled opioid ligand and varying concentrations of leuphasyl. Binding affinity (Ki) is determined by measuring displacement of the radiolabeled ligand. Selectivity profiling against mu and kappa opioid receptors is performed to confirm specificity.
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| Cell Assay |
Cellular assays for leuphasyl are performed using cells expressing delta opioid receptors. Cells are treated with the compound at various concentrations, and downstream signaling such as cAMP inhibition or GTPγS binding is measured. EC₅₀ values for receptor activation are determined from dose-response curves. Acetylcholine release assays can be performed using neuronal cultures or brain slices to assess inhibition of neurotransmitter release.
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| Animal Protocol |
In vivo animal models for leuphasyl would be required to assess its therapeutic potential. Based on its mechanism as a delta opioid agonist, relevant models could include pain models (e.g., hot plate, tail flick, formalin test) and models of mood disorders. The compound would be administered via appropriate routes, and behavioral and physiological parameters would be measured.
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| ADME/Pharmacokinetics |
Leuphasyl has a molecular weight of 569.28 g/mol and a molecular formula of C₂₉H₃₉N₅O₇. CAS number is 64963-01-5. Melting point is 160-163.5°C. Density is 1.257±0.06 g/cm³. Appearance is a solid powder. Purity is ≥98%. Storage conditions: powder at -20°C. The compound is supplied for research use only.
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| Toxicity/Toxicokinetics |
Detailed toxicological data for leuphasyl are not extensively reported in the available literature. As a research compound, its safety profile would need to be established through standard preclinical toxicity assessments. The compound is supplied for research use only and is not for human consumption. Given its mechanism as a delta opioid agonist, potential side effects may include those associated with opioid receptor modulation.
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| Additional Infomation |
Leuphasyl is also known as Pentapeptide-18, [D-Ala2]-Leucine enkephalin, and YdAGFL. It is a synthetic pentapeptide that acts as a delta opioid agonist. The compound inhibits the release of acetylcholine and inhibits muscle contraction. It is a long-acting leucine brain non-peptide that resists degradation. Leuphasyl is used in research applications studying opioid receptor signaling and neurotransmitter release. It is also used in cosmetics as an INCI name. It is for research use only.
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| Molecular Formula |
C29H39N5O7
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|---|---|
| Molecular Weight |
569.65
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| Exact Mass |
569.284
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| CAS # |
64963-01-5
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| PubChem CID |
10099522
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
991.9±65.0 °C at 760 mmHg
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| Flash Point |
553.7±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.582
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| LogP |
2.42
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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 |
15
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| Heavy Atom Count |
41
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| Complexity |
885
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C[C@H](C(=O)NCC(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](CC(C)C)C(=O)O)NC(=O)[C@H](CC2=CC=C(C=C2)O)N
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| InChi Key |
ZHUJMSMQIPIPTF-JMBSJVKXSA-N
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| InChi Code |
InChI=1S/C29H39N5O7/c1-17(2)13-24(29(40)41)34-28(39)23(15-19-7-5-4-6-8-19)33-25(36)16-31-26(37)18(3)32-27(38)22(30)14-20-9-11-21(35)12-10-20/h4-12,17-18,22-24,35H,13-16,30H2,1-3H3,(H,31,37)(H,32,38)(H,33,36)(H,34,39)(H,40,41)/t18-,22+,23+,24+/m1/s1
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| Chemical Name |
(2S)-2-[[(2S)-2-[[2-[[(2R)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoic acid
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| Synonyms |
NSC-374895; NSC 374895; Leuphasyl
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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 : ~50 mg/mL (~87.77 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (87.77 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7555 mL | 8.7773 mL | 17.5546 mL | |
| 5 mM | 0.3511 mL | 1.7555 mL | 3.5109 mL | |
| 10 mM | 0.1755 mL | 0.8777 mL | 1.7555 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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