2. Metabolic Enzyme/Protease Neuronal Signaling GPCR/G Protein Stem Cell/Wnt MAPK/ERK Pathway PI3K/Akt/mTOR Vitamin D Related/Nuclear Receptor
  3. Enteropeptidase Aminopeptidase Opioid Receptor ERK mTOR Androgen Receptor
  4. Sialorphin TFA

Sialorphin TFA 是一种中性内肽酶 (NEP) 和氨肽酶 N (APN) 抑制剂，可响应雄激素信号。Sialorphin TFA 能阻断内源性阿片肽降解并与 μ-、δ-、κ-阿片受体相互作用。Sialorphin TFA 通过诱导细胞周期阻滞、提高 ERK1/2 活性，降低 mTOR、4E-BP1、p70S6K 的磷酸化水平，来调节 ERK/mTOR 信号通路；从而，Sialorphin TFA 对结直肠癌、胶质瘤和前列腺癌细胞具有抗增殖活性，且无细胞毒性。此外，Sialorphin TFA 还具有抗伤害性感受反应、调节性行为、松弛阴茎海绵体平滑肌，以及减轻实验性结肠炎。Sialorphin TFA 还是一种铜 (II) 离子结合配体。Sialorphin TFA 已应用于癌症、疼痛管理及炎症性肠病等相关领域的机制研究中。

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Custom Peptide Synthesis

Sialorphin TFA

Sialorphin TFA Chemical Structure

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规格 价格 是否有货 数量
5 mg ￥440
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10 mg ￥720
In-stock
25 mg ￥1440
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100 mg   询价  

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Customer Review

Other Forms of Sialorphin TFA:

Sialorphin TFA 相关抗体

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CD13 LTA4H

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1][2][3][4][5].

IC50 & Target

ERK1

 

ERK2

 

μ Opioid Receptor/MOR

 

κ Opioid Receptor/KOR

 

δ Opioid Receptor/DOR

 

体外研究
(In Vitro)

Sialorphin (10 μM；20 min) 可抑制大鼠脊髓切片中 Met -脑啡肽 (ME) 的分解，抑制率达 70%-96%，同时能抑制脊髓组织 (膜或切片) 中 3H-SP 的水解，抑制率为 55%，其抑制 3H-SP 分解的 IC50 为 3.9×10-7 M[1]。
Sialorphin (400 nM-4000 nM；10-20 min) 对大鼠肾细胞膜中 3H-SP 的内肽酶水解具有浓度依赖性抑制作用，IC50 为 1 μM，且为竞争性抑制，与磷酰胺素抑制效果相当[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Sialorphin TFA 相关抗体:

ELISA Assay[1]

Cell Line: Rat spinal cord slice cells
Concentration: 4, 10 μM
Incubation Time: 20 min
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.
体内研究
(In Vivo)

Sialorphin TFA (0.3-10 mg/kg; i.p.; 每日 2 次; 3 d) 可显著减轻小鼠中 TNBS 诱导的急性结肠炎，减轻宏观损伤、溃疡、结肠壁增厚及降低 MPO 活性；该作用由 μ- 和 κ-阿片受体介导[2]。
Sialorphin TFA (1 mg/kg; i.p.; 每日 2 次; 7 d) 可显著减轻小鼠中由 TNBS 诱导的慢性复发性结肠炎[2]。
Sialorphin TFA (1 mg/kg; i.p.; 每日 2 次; 7 d) 在 40 KD DSS (HY-116282C) 诱导的小鼠结肠炎模型中未表现出抗炎活性[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c (male, 6-8 weeks old, 22-26 g, intracolonic instillation of TNBS to induce acute colitis)[2]
Dosage: 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: i.p.; twice daily; 3 days
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.
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]
Dosage: 1 mg/kg
Administration: i.p.; twice daily; 7 days
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.
分子量

650.69 (free base)

Formula

C26H42N12O8·xC2HF3O2
性状

固体

Sequence

Gln-His-Asn-Pro-Arg
Sequence Shortening

QHNPR
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

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)

溶解性数据
细胞实验： 

H2O 中的溶解度 : 100 mg/mL (超声助溶)

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
纯度 & 产品资料
参考文献

Sialorphin TFA 相关分类

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SialorphinEnteropeptidaseAminopeptidaseOpioid ReceptorERKmTORAndrogen ReceptorEnterokinaseTransmembrane serine protease 15TMPRSS15 Extracellular signal regulated kinasesMammalian target of Rapamycincopper(II) ionδ-opioid receptorsglioma cancer cellscolorectal cancer cellsaminopeptidase N (APN)μ-opioid receptorsκ-opioid receptorsNeutral endopeptidase (NEP)prostate cancer cellsnormal human fibroblastsInhibitorinhibitorinhibit

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