2. Metabolic Enzyme/Protease Apoptosis
  3. Neprilysin Glutathione Peroxidase
  4. Sialorphin

Sialorphin 是一种 NEP 和 APN 抑制剂。Sialorphin 能有效抑制 NEP 对 Substance P (HY-P0201) 和甲硫氨酸脑啡肽的降解。Sialorphin 具有镇痛、调节雄性大鼠性行为、减轻结肠炎等多种生物活性。Sialorphin 对部分肿瘤细胞也具有较弱的毒性。Sialorphin 可用于疼痛、炎症性肠病和肿瘤等疾病的研究。

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Custom Peptide Synthesis

Sialorphin

Sialorphin Chemical Structure

CAS No. : 131748-26-0

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Sialorphin 的其他形式现货产品:

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Sialorphin 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Sialorphin is an inhibitor of NEP and APN. Sialorphin potently inhibits the degradation of Substance P (HY-P0201) and methionine enkephalin by NEP. Sialorphin exhibits multiple biological activities such as analgesia, regulation of sexual behavior in male rats, and alleviation of colitis. Sialorphin also shows weak toxicity against certain tumor cells. Sialorphin can be used in the research of diseases including pain, inflammatory bowel disease, and tumors[1][2][3][4].

体外研究
(In Vitro)

Sialorphin (0-10 μM) 可抑制大鼠肾细胞膜和脊髓膜对 Substance P (HY-P0201) 的降解作用，其 IC50 分别为 1 和 0.39 μM[1]。
Sialorphin (50-1000 μM；48 h) 对 PC3 人前列腺癌细胞表现出细胞毒性 (LC50: 185 μM)，对 LN18 人脑胶质瘤细胞在浓度高达 1000 μM 时仍未达到 LC50，对 A549、HCT116 和 B16-F10 细胞无显著毒性[3]。

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

Sialorphin 相关抗体:
体内研究
(In Vivo)

Sialorphin (50-100 μg/kg；静脉注射；单剂量) 在雄性大鼠针刺疼痛模型中显著减少疼痛相关发声与逃避行为，增加针刺区域的跨区和直立探索行为[1]。
Sialorphin (200 μg/kg；静脉注射；单剂量) 在雄性大鼠福尔马林疼痛模型中显著缩短舔爪时长，抑制急性化学性伤害性疼痛反应[1]。
Sialorphin (0.3-3 mg/kg；腹腔注射；每日 2 次；3-7 天) 可缓解小鼠中由 TNBS 诱导的结肠炎[2]。
Sialorphin (1 mg/kg；腹腔注射；每日 2 次；7 天) 对 DSS (HY-116282C) 诱导的小鼠结肠炎无作用[2]。
Sialorphin (0.3-3 µg/kg；静脉注射；单次给药) 可呈剂量依赖性调节雄性大鼠的性行为[4]。

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

Animal Model: Wistar rats (male, 6 weeks old, 350-400 g)[1]
Dosage: 200 μg/kg
Administration: i.v.; single dose
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.
Animal Model: BALB/c (male, 6-8 weeks old, 22-26 g, TNBS-induced acute colitis)[2]
Dosage: 0.3, 1, 3, 10 mg/kg
Administration: i.p.; twice daily; 3 days
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.
Animal Model: BALB/c (male, 6-8 weeks old, 22-26 g, TNBS-induced established colitis)[2]
Dosage: 1 mg/kg
Administration: i.p.; twice daily; 4 days
Result: Decreased macroscopic score, ulcer score, colonic wall thickness, and MPO activity.
Animal Model: BALB/c (male, 6-8 weeks old, 22-26 g, TNBS-induced chronic relapsing colitis)[2]
Dosage: 1 mg/kg
Administration: i.p.; twice daily; 7 days
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.
Animal Model: Wistar/AF (male, 300-320 g)[4]
Dosage: 0.3, 1, 3 µg/kg
Administration: i.v.; single dose
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.
分子量

650.69

Formula

C26H42N12O8
CAS 号
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

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Sialorphin 相关分类

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  • 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:

Sialorphin131748-26-0NeprilysinGlutathione PeroxidaseNeutral endopeptidaseNEPCluster of differentiation 10CD10prostate cancer cellsδ-opioid receptorμ-opioid receptorrat spinal tissueaminopeptidase Nglioblastoma cellssubstance PInhibitorinhibitorinhibit

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