| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
Spinorphin inhibits enkephalin-degrading enzymes, including aminopeptidase, dipeptidyl aminopeptidase III, angiotensin-converting enzyme (ACE), and enkephalinase (neprilysin). For monkey brain enzymes, its IC50s are 3.3, 1.4, 2.4, and 10 μg/mL, respectively. By inhibiting these enzymes, Spinorphin prevents the degradation of endogenous enkephalins, thereby potentiating opioid signaling. It is selective for these enzymes over human serum aminopeptidase A and various porcine kidney enzymes.
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| ln Vitro |
In vitro, Spinorphin inhibits chemotaxis, production of reactive oxygen species (ROS), and exocytosis of glucuronidase and collagenase in polymorphonuclear neutrophils (PMNs). It potentiates enkephalin-induced action potentials in rat hippocampal slices. Spinorphin inhibited cytoplasmic Ca2+ ([Ca2+]i) transients evoked by depolarization. It does not show inhibitory activity toward enkephalin-degrading enzymes from kidney or blood.
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| ln Vivo |
In vivo, Spinorphin (5 μg/animal) enhances the antinociceptive effects of Leu-enkephalin in mice. It possesses an antinociceptive effect and potentiates enkephalin-induced anti-allodynic effects. Spinorphin has been studied for its potential in pain relief research. Its in vivo efficacy is attributed to its ability to inhibit enkephalin-degrading enzymes and potentiate endogenous opioid signaling.
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| Enzyme Assay |
In vitro enzyme assays for Spinorphin typically involve measuring the inhibition of enkephalin-degrading enzymes such as aminopeptidase, dipeptidyl aminopeptidase III, ACE, and enkephalinase. IC50 values for monkey brain enzymes are 3.3, 1.4, 2.4, and 10 μg/mL, respectively. The compound's selectivity is assessed by testing against human serum aminopeptidase A and various porcine kidney enzymes. These assays confirm its mechanism of action as an enkephalin-degrading enzyme inhibitor.
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| Cell Assay |
In vitro cellular assays for Spinorphin typically involve treating polymorphonuclear neutrophils (PMNs) with the compound and measuring chemotaxis, ROS production, and exocytosis of glucuronidase and collagenase. Its effects on cytoplasmic Ca2+ transients evoked by depolarization can also be assessed. Spinorphin potentiates enkephalin-induced action potentials in rat hippocampal slices. These cell-based studies demonstrate its immunomodulatory and neuromodulatory effects.
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| Animal Protocol |
In vivo animal models for Spinorphin typically involve studying its antinociceptive effects in mice. Spinorphin (5 μg/animal) enhances the antinociceptive effects of Leu-enkephalin in mice. It potentiates enkephalin-induced anti-allodynic effects. Animal models may also be used to study its effects on pain and inflammation. Doses and administration routes are optimized based on the specific model and experimental endpoints.
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| ADME/Pharmacokinetics |
Spinorphin has a molecular formula of C45H64N8O10 and a molecular weight of 877.04. Its sequence is Leu-Val-Val-Tyr-Pro-Trp-Thr (LVVYPWT). The compound is soluble in DMF (30 mg/mL) and DMSO (30 mg/mL). It is typically stored at room temperature for shipping. Spinorphin is an endogenous neuropeptide belonging to the opioid hemorphin family.
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| Toxicity/Toxicokinetics |
Spinorphin is an endogenous peptide inhibitor of enkephalin-degrading enzymes. As with any peptide, potential toxicity may include immunogenicity and effects on opioid signaling pathways. The compound's safety profile should be evaluated in preclinical toxicology studies. Spinorphin is for research use only and is not approved for human therapeutic use. It represents a valuable tool for studying enkephalin degradation and pain modulation.
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| References | |
| Additional Infomation |
Spinorphin is an oligopeptide.
Spinorphin (CAS# 137201-62-8) is a heptapeptide (Leu-Val-Val-Tyr-Pro-Trp-Thr) and a potent inhibitor of enkephalin-degrading enzymes from the spinal cord or brain. It inhibits aminopeptidase, dipeptidyl aminopeptidase III, ACE, and enkephalinase, with IC50s of 3.3, 1.4, 2.4, and 10 μg/mL, respectively. Spinorphin potentiates enkephalin-induced antinociceptive effects in mice. It is an endogenous peptide belonging to the opioid hemorphin family. The compound is for research use only and not for human therapeutic use. |
| Molecular Formula |
C45H64N8O10
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|---|---|
| Molecular Weight |
877.05
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| Exact Mass |
876.475
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| CAS # |
137201-62-8
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| PubChem CID |
3081832
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| Sequence |
Leu-Val-Val-Tyr-Pro-Trp-ThrLVVYPWT
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| SequenceShortening |
LVVYPWT
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.277g/cm3
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| Boiling Point |
1256.3ºC at 760 mmHg
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| Flash Point |
713.6ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.598
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| LogP |
3.817
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
21
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| Heavy Atom Count |
63
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| Complexity |
1590
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| Defined Atom Stereocenter Count |
8
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| SMILES |
O=C([C@H](CC1C=CC(=CC=1)O)N([H])C([C@H](C(C)C)N([H])C([C@H](C(C)C)N([H])C([C@H](CC(C)C)N([H])[H])=O)=O)=O)N1CCC[C@H]1C(N([H])[C@H](C(N([H])[C@H](C(=O)O)[C@@H](C)O)=O)CC1=CN([H])C2=CC=CC=C12)=O
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| InChi Key |
BXIFNVGZIMFBQB-DYDSHOKNSA-N
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| InChi Code |
InChI=1S/C45H64N8O10/c1-23(2)19-31(46)39(56)50-37(25(5)6)43(60)51-36(24(3)4)42(59)49-34(20-27-14-16-29(55)17-15-27)44(61)53-18-10-13-35(53)41(58)48-33(40(57)52-38(26(7)54)45(62)63)21-28-22-47-32-12-9-8-11-30(28)32/h8-9,11-12,14-17,22-26,31,33-38,47,54-55H,10,13,18-21,46H2,1-7H3,(H,48,58)(H,49,59)(H,50,56)(H,51,60)(H,52,57)(H,62,63)/t26-,31+,33+,34+,35+,36+,37+,38+/m1/s1
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| Chemical Name |
(2S,3R)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-3-methylbutanoyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoic acid
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| Synonyms |
Leu-val-val-tyr-pro-trp-thr; Spinorphin
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1402 mL | 5.7009 mL | 11.4019 mL | |
| 5 mM | 0.2280 mL | 1.1402 mL | 2.2804 mL | |
| 10 mM | 0.1140 mL | 0.5701 mL | 1.1402 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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