製品番号: HY-P11642A

Sialorphin TFA

カスタマーレビュー

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

分子式: C₂₆H₄₂N₁₂O₈·xC₂HF₃O₂
分子量:650.69 (free base)

保管条件:

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)

Sialorphin TFA 構造式

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
溶剤 & 溶解度
- 体外
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

ERK1

ERK2

μ Opioid Receptor/MOR

κ Opioid Receptor/KOR

δ Opioid Receptor/DOR

Aminopeptidase アイソフォーム固有の製品をすべて表示 :

CD13
LTA4H

Opioid Receptor アイソフォーム固有の製品をすべて表示 :

ERK アイソフォーム固有の製品をすべて表示 :

mTOR アイソフォーム固有の製品をすべて表示 :

体外実験

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.

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.

体内実験

Sialorphin TFA (0.3-10 mg/kg; i.p.; twice daily; 3 days) at doses of 0.3, 1, and 3 mg/kg significantly attenuates acute TNBS-induced colitis in Mus musculus, as measured by reduced macroscopic damage, ulceration, colonic wall thickening, and MPO activity^[2].
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.

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.

化学情報

性状 Solid
分子量 650.69 (free base)
分子式 C₂₆H₄₂N₁₂O₈·xC₂HF₃O₂
配列

Gln-His-Asn-Pro-Arg
シーケンスの短縮

QHNPR
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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)

溶剤 & 溶解度

体外:

H₂O : 100 mg/mL (Need ultrasonic)

View the Complete Stock Solution Preparation Table

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (286 KB)
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)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[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]

[3]. Mizerska-Kowalska M, et al. Neutral endopeptidase (NEP) inhibitors–thiorphan, sialorphin, and its derivatives exert anti-proliferative activity towards colorectal cancer cells in vitro[J]. Chemico-Biological Interactions, 2019, 307: 105-115.

[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]

[5]. Kamysz E, et al. Sialorphin and its analog as ligands for copper (II) ions[J]. Polyhedron, 2013, 55: 216-224.

Calculators

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

製品名:
製品番号:
数量:
日本の代理先をお選びください:

製品名:
CAS 番号:
生物種:
純度:
数量:

Sialorphin TFA

Peptide Library

Aminopeptidase アイソフォーム固有の製品をすべて表示

Opioid Receptor アイソフォーム固有の製品をすべて表示

ERK アイソフォーム固有の製品をすべて表示

mTOR アイソフォーム固有の製品をすべて表示