Sialorphin TFA
Based on 1 Customer Validation
Sialorphin TFA is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin TFA blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin TFA 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 TFA exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin TFA also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin TFA is also a copper (II) ion-binding ligand. Sialorphin TFA has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease.
For research use only. We do not sell to patients.
- Formula: C26H42N12O8·xC2HF3O2
- Molecular Weight:650.69 (free base)
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Storage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All Opioid Receptor Isoforms
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Biological Activity
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ERK1 |
ERK2 |
μ Opioid Receptor/MOR |
κ Opioid Receptor/KOR |
δ Opioid Receptor/DOR |
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.
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Cell Line:Rat spinal cord slice cells
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Concentration:4, 10 μM
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Incubation Time:20 min
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Result:Effectively prevented the breakdown of exogenous ME by spinal enkephalinase ex vivo, with an inhibition rate ranging from 70% to 96%.
Inhibited the endoproteolysis of 3H-SP by rat renal membranes with a correlation coefficient (r) of 0.970.
At 4 μM, inhibited 60% of the specific SP - hydrolyzing activity of rat kidney tissue, which was as effective as phosphoramidon.
Sialorphin TFA (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 TFA (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:BALB/c (male, 6-8 weeks old, 22-26 g, intracolonic instillation of TNBS to induce acute colitis)[2]
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Dosage:0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
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Administration:i.p.; twice daily; 3 days
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Result:Significantly reduced macroscopic colonic damage scores, ulcer scores, colonic wall thickness, and myeloperoxidase (MPO) activity at 0.3, 1, and 3 mg/kg compared to TNBS-only controls.
Significantly reduced ulcer scores and colonic wall thickness, but did not reduce MPO activity, and only non-significantly reduced total macroscopic scores (p=0.09) at 10 mg/kg compared to TNBS-only controls.
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Animal Model:BALB/c mice with Inflammatory bowel disease (male, 6-8 weeks old, 22-26 g, 4% wt/vol DSS in drinking water to induce 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:Significantly reduced macroscopic colonic damage scores, ulcer scores, colonic wall thickness, and MPO activity compared to TNBS-only controls.
Reduced body weight loss, decreased colon expression of pro-inflammatory cytokines TNFα and IL-1β, and lowered histological colon damage scores (reduced mucosal architecture destruction, smooth muscle thickening, crypt abscesses, and cellular infiltration) compared to TNBS-only controls.
Did not reduce any evaluated parameters of colitis, including macroscopic damage scores, colon weight, colon length, MPO activity, or body weight loss, compared to DSS-only controls.
Chemical Information
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Appearance Solid
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Molecular Weight 650.69 (free base)
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Formula C26H42N12O8·xC2HF3O2
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Sequence
Gln-His-Asn-Pro-Arg
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Sequence Shortening
QHNPR
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H2O : 100 mg/mL (Need ultrasonic)
Purity & Documentation
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Data Sheet (286 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Sialorphin TFA Related Classifications
HY-P11642A Related Classifications
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- Sialorphin
- Enteropeptidase
- Aminopeptidase
- Opioid Receptor
- ERK
- mTOR
- Androgen Receptor
- copper(II) ion
- δ-opioid receptors
- glioma cancer cells
- colorectal cancer cells
- aminopeptidase N (APN)
- μ-opioid receptors
- κ-opioid receptors
- Neutral endopeptidase (NEP)
- prostate cancer cells
- normal human fibroblasts
- Inhibitor
- inhibitor
- inhibit