Spinorphin (Synonyms: Leu-Val-Val-Tyr-Pro-Trp-Thr, LVVYPWT) |
Catalog No.GC16894
One-Click Copy Product Info
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A peptide inhibitor of enkephalin-degrading enzymes
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 137201-62-8
Sample solution is provided at 25 µL, 10mM.
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Spinorphin is an endogenous inhibitor of enkephalin-degrading enzymes (aminopeptidase, dipeptidyl aminopeptidase III, angiotensin-converting enzyme and enkephalinase) [1]. Also, it is a potent antagonist of human P2X3 receptor and the N-formylpeptide receptor subtype FPR with IC50 value of 8.3 pM for P2X3 receptor[2][3].
Enkephalin degrading enzymes are a series of enzymes that hydrolyze enkephalins, which play an important role in management of blood pressure, pain, hypertension and cardiovascular diseases.
In human embryonic kidney (HEK) 293 cells transfected with mouse FPR, spinorphin induced a typical rise in the intracellular Ca2+ concentration with EC50 of 128 μM. Also, in normal mouse neutrophils, Spinorphin induced calcium flux in a dose-dependent way. While the neutrophils from mice deficient in the fMLF receptor subtype FPR didn’t response [3].
In mice, intrathecal administration of spinorphin inhibited the allodynia induced by intrathecal nociceptin in a dose-dependent way. Furthermore, spinorphin enhanced the inhibitory effect of enkephalin on allodynia induced by nociceptin [4].
References:
[1]. Nishimura K, Hazato T. Isolation and identification of an endogenous inhibitor of enkephalin-degrading enzymes from bovine spinal cord. Biochem Biophys Res Commun, 1993, 194(2): 713-719.
[2]. Jung KY, Moon HD, Lee GE, et al. Structure-activity relationship studies of spinorphin as a potent and selective human P2X(3) receptor antagonist. J Med Chem, 2007, 50(18): 4543-4547.
[3]. Liang TS, Gao JL, Fatemi O, et al. The endogenous opioid spinorphin blocks fMet-Leu-Phe-induced neutrophil chemotaxis by acting as a specific antagonist at the N-formylpeptide receptor subtype FPR. J Immunol, 2001, 167(11): 6609-6614.
[4]. Honda M, Okutsu H, Matsuura T, et al. Spinorphin, an endogenous inhibitor of enkephalin-degrading enzymes, potentiates leu-enkephalin-induced anti-allodynic and antinociceptive effects in mice. Jpn J Pharmacol, 2001, 87(4): 261-267.
| Cas No. | 137201-62-8 | SDF | |
| Synonymes | Leu-Val-Val-Tyr-Pro-Trp-Thr, LVVYPWT | ||
| Chemical Name | 2-(2-(1-(2-(2-(2-(2-amino-4-methylpentanamido)-3-methylbutanamido)-3-methylbutanamido)-3-(4-hydroxyphenyl)propanoyl)pyrrolidine-2-carboxamido)-3-(1H-indol-3-yl)propanamido)-3-hydroxybutanoic acid | ||
| Canonical SMILES | CC(C)CC(C(=O)NC(C(C)C)C(=O)NC(C(C)C)C(=O)NC(CC1=CC=C(C=C1)O)C(=O)N2CCCC2C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(C(C)O)C(=O)O)N | ||
| Formula | C45H64N8O10 | M.Wt | 877.05 |
| Solubility | DMF: 30 mg/ml,DMSO: 30 mg/ml | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.1402 mL | 5.7009 mL | 11.4019 mL |
| 5 mM | 228 μL | 1.1402 mL | 2.2804 mL |
| 10 mM | 114 μL | 570.1 μL | 1.1402 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)