Sialorphin
Sialorphin is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin is also a copper (II) ion-binding ligand. Sialorphin has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease.
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- CAS. Nr.: 131748-26-0
- Formel: C26H42N12O8
- Molecular Weight:650.69
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Sialorphin (10 μM; 20 min) inhibits the degradation of Met-enkephalin (ME) in rat spinal cord slices with an inhibition rate of 70%-96%, and simultaneously inhibits the hydrolysis of 3H-SP in spinal cord tissues (membranes or slices) with an inhibition rate of 55%. Its IC50 for inhibiting 3H-SP degradation is 3.9×10-7 M[1].
Sialorphin (400 nM-4000 nM; 10-20 min) exerts a concentration-dependent inhibitory effect on endopeptidase-mediated hydrolysis of 3H-SP in rat renal cell membranes, with an IC50 of 1 μM. This inhibition is competitive and comparable in efficacy to that of phosphoramidon[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Sialorphin (1 mg/kg; i.p.; twice daily; 7 days) significantly attenuates chronic, relapsing TNBS-induced colitis in mice, as measured by reduced clinical, biochemical, histological, and cytokine markers of inflammation[2].
Sialorphin (1 mg/kg; i.p.; twice daily; 7 days) does not exhibit anti-inflammatory activity in DSS-induced colitis in mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats (male, 6 weeks old, 350-400 g)[1]
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Dosage:200 μg/kg
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Administration:i.v.; single dose
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Result:Reduced paw licking time from 106.3 s to 66.3 s.
Abolished this effect when pretreated with μ-opioid receptor or δ-opioid receptor antagonist.
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Animal Model:BALB/c (male, 6-8 weeks old, 22-26 g, TNBS-induced acute colitis)[2]
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Dosage:0.3, 1, 3, 10 mg/kg
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Administration:i.p.; twice daily; 3 days
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Result:Decreased macroscopic score, ulcer score, colonic wall thickness, and myeloperoxidase (MPO) activity at 0.3, 1, and 3 mg/kg.
Reduced ulcer score and colonic wall thickness at 10 mg/kg, with no reduction in MPO activity and non-statistically significant reduction in macroscopic score at 10 mg/kg.
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Animal Model:BALB/c (male, 6-8 weeks old, 22-26 g, TNBS-induced established colitis)[2]
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Dosage:1 mg/kg
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Administration:i.p.; twice daily; 4 days
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Result:Decreased macroscopic score, ulcer score, colonic wall thickness, and MPO activity.
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Animal Model:BALB/c (male, 6-8 weeks old, 22-26 g, TNBS-induced chronic relapsing colitis)[2]
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Dosage:1 mg/kg
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Administration:i.p.; twice daily; 7 days
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Result:Decreased macroscopic score, ulcer score, colonic wall thickness, MPO activity, body weight loss, and expression of pro-inflammatory cytokines TNFα and IL-1β.
Reduced histological damage score.
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Animal Model:Wistar/AF (male, 300-320 g)[4]
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Dosage:0.3, 1, 3 µg/kg
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Administration:i.v.; single dose
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Result:Increased the occurrence of intromissions across the successive ejaculatory sequences.
Significantly reduces the ejaculation frequency at the highest dose of 3 μg/kg, and all doses promote the frequency of intromissions before ejaculation and investigatory behavior toward female rats during the post-ejaculatory interval, while stimulating the level of sexual arousal or motivation in rats.
Chemical Information
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CAS. Nr. 131748-26-0
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Molecular Weight 650.69
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Formel C26H42N12O8
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Sequence
Gln-His-Asn-Pro-Arg
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Sequence Shortening
QHNPR
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Rougeot C, et al. Sialorphin, a natural inhibitor of rat membrane-bound neutral endopeptidase that displays analgesic activity. Proc Natl Acad Sci U S A. 2003;100(14):8549-8554. [Content Brief]
[2]. Salaga M, et al. Systemic Administration of Sialorphin Attenuates Experimental Colitis in Mice via Interaction With Mu and Kappa Opioid Receptors. J Crohns Colitis. 2017;11(8):988-998. [Content Brief]
[4]. Kamysz E, et al. Antitumor activity of opiorphin, sialorphin and their conjugates with a peptide klaklakklaklak. J Pept Sci. 2016;22(11-12):723-730. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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