Tyr-Gly-Gly-Phe-Met-OH (Met-Enkephalin)
(Synonyms: 蛋氨酸脑啡肽; Met-Enkephalin; Methionine enkephalin) 目录号 : GC30816
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Tyr-Gly-Gly-Phe-Met-OH (Met-Enkephalin)是一种内源性阿片肽，作为δ阿片受体激动剂，EC50值为1.03nM。
Cas No.:58569-55-4
Sample solution is provided at 25 µL, 10mM.
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Tyr-Gly-Gly-Phe-Met-OH (Met-Enkephalin) is an endogenous opioid that acts as the δ opioid receptor with an EC50 value of 1.03nM[1]. Tyr-Gly-Gly-Phe-Met-OH can induce changes in macrophage function, stimulate the phagocytic activity of macrophages, and enhance the production of cytokines by macrophages[2]. Tyr-Gly-Gly-Phe-Met-OH can serve as a biomarker for stress-induced changes in the brain in mouse models[3].
In vitro, Tyr-Gly-Gly-Phe-Met-OH treatment (0.1nM) for 24h combined with IFN-γ caused an increase in IL-6 release from the cultured murine macrophages[4]. Tyr-Gly-Gly-Phe-Met-OH (0.1nM; 1h) enhanced the H2O2 release in macrophages pretreated with 25nM phorbol myristate acetate (PMA) [5]. Treatment with 12.5mg/ml Tyr-Gly-Gly-Phe-Met-OH for 48 hours significantly inhibited the proliferation of B16 cells and induced cell cycle arrest[6].
In vivo, Tyr-Gly-Gly-Phe-Met-OH treatment via intraperitoneal injection at a dose of 10mg/kg/day for 28 days significantly reduced the tumor volume in mice with the xenograft of MG-63 cells, without affecting body weight [7]. Tyr-Gly-Gly-Phe-Met-OH treatment (20mg/kg/day; i.p.) for 21 days inhibited tumor growth by enhancing the immunogenicity and recognition of MC38 cells in colorectal tumor-bearing mice and efficiently suppressed the mRNA expression of genes encoding inflammatory cytokines in the tumor tissues of mice [8].
References:
[1] Nagase H, Osa Y, Nemoto T, et al. Design and synthesis of novel delta opioid receptor agonists and their pharmacologies[J]. Bioorganic & medicinal chemistry letters, 2009, 19(10): 2792-2795.
[2]Zhao D, Plotnikoff N, Griffin N, et al. Methionine enkephalin, its role in immunoregulation and cancer therapy[J]. International immunopharmacology, 2016, 37: 59-64.
[3] Nabeshima T, Katoh A, Wada M, et al. Stress-induced changes in brain Met-enkephalin, Leu-enkephalin and dynorphin concentrations[J]. Life sciences, 1992, 51(3): 211-217.
[4] Kowalski J, Makowiecka K, Belowski D, et al. Augmenting effect of methionine-enkephalin on interleukin-6 production by cytokine-stimulated murine macrophages[J]. Neuropeptides, 2000, 34(3-4): 187-192.
[5] Stanojević S, Vujić V, Mitić K, et al. Methionine-enkephalin modulation of hydrogen peroxide (H2O2) release by rat peritoneal macrophages involves different types of opioid receptors[J]. Neuropeptides, 2008, 42(2): 147-158.
[6] Wang D M, Jiao X, Plotnikoff N P, et al. Killing effect of methionine enkephalin on melanoma in vivo and in vitro[J]. Oncology Reports, 2017, 38(4): 2132-2140.
[7] Huang H, Wang X, Zhang S, et al. In vitro and in vivo killing effects of methionine enkephalin on osteosarcoma[J]. International Immunopharmacology, 2023, 125: 111226.
[8] Wang X, Li S, Yan S, et al. Methionine enkephalin inhibits colorectal cancer by remodeling the immune status of the tumor microenvironment[J]. International Immunopharmacology, 2022, 111: 109125.
Tyr-Gly-Gly-Phe-Met-OH (Met-Enkephalin)是一种内源性阿片肽，作为δ阿片受体激动剂，EC50值为1.03nM[1]。Tyr-Gly-Gly-Phe-Met-OH可诱导巨噬细胞功能改变，刺激巨噬细胞的吞噬活性，并增强巨噬细胞产生细胞因子[2]。Tyr-Gly-Gly-Phe-Met-OH在小鼠模型中可作为应激诱导脑内变化的生物标志物[3]。
在体外，使用0.1nM的Tyr-Gly-Gly-Phe-Met-OH联合IFN-γ处理24小时，导致培养的小鼠巨噬细胞中IL-6的释放增加[4]。Tyr-Gly-Gly-Phe-Met-OH（0.1nM；1小时）增强了经25nM phorbol myristate acetate（PMA）预处理的巨噬细胞中H2O2的释放[5]。使用12.5mg/ml的Tyr-Gly-Gly-Phe-Met-OH处理48小时，显著抑制了B16细胞的增殖并诱导了细胞周期阻滞[6]。
在体内，每日腹腔注射10mg/kg剂量的Tyr-Gly-Gly-Phe-Met-OH，持续28天，显著降低了携带MG-63细胞异种移植瘤的小鼠的肿瘤体积，且未影响体重[7]。每日腹腔注射20mg/kg剂量的Tyr-Gly-Gly-Phe-Met-OH，持续21天，通过增强结直肠癌荷瘤小鼠中MC38细胞的免疫原性和识别能力来抑制肿瘤生长，并有效抑制了小鼠肿瘤组织中编码炎症细胞因子基因的mRNA表达[8]。
| Cell experiment [1]: | |
Cell lines | B16 cells |
Preparation Method | B16 cells were cultured in RPMI-1640 medium supplemented with 10% fetal bovine serum (FBS) and antibiotics (penicillin 100U/ml, streptomycin 0.1mg/ml) under normal conditions (5% CO2 with 95% humidified air). B16 mouse melanoma cells (5×104 per well) were inoculated in 96-well cell culture plate and incubated at 37°C with 5% CO2 for 24h. The cells were treated with different concentrations of Tyr-Gly-Gly-Phe-Met-OH (0, 2.5, 5, 10, 12.5 and 15mg/ml) for 24, 48, 72, and 96h, respectively, and cell viability was measured. |
Reaction Conditions | 0, 2.5, 5, 10, 12.5, and 15mg/ml; 24, 48, 72, and 96h |
Applications | Tyr-Gly-Gly-Phe-Met-OH treatment reduced the cell viability of B16 cells in a dose- and time-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male BABL/C nude mice |
Preparation Method | The 6-week-old male BABL/C nude mice were housed at 22-25°C and 20-25% humidity under a 12h light/dark cycle, and provided free access to food and water. After 5 days of acclimatization, the MG-63 cell suspension was subcutaneously injected into nude mice (5×106 cells), which were randomly divided into two groups (n=6 for each group): control and Tyr-Gly-Gly-Phe-Met-OH. Mice in the control and Tyr-Gly-Gly-Phe-Met-OH groups were intraperitoneally injected with saline and Tyr-Gly-Gly-Phe-Met-OH (10mg/kg/day), respectively. The administration period lasted for 28 days, and the tumor volume of the mice was monitored every three days. |
Dosage form | 10mg/kg/day for 28 days; i.p. |
Applications | Tyr-Gly-Gly-Phe-Met-OH treatment significantly reduced the tumor volume in mice with a xenograft of MG-63 cells. |
References: | |
| Cas No. | 58569-55-4 | SDF | |
| 别名 | 蛋氨酸脑啡肽; Met-Enkephalin; Methionine enkephalin | ||
| Canonical SMILES | Tyr-Gly-Gly-Phe-Met | ||
| 分子式 | C27H35N5O7S | 分子量 | 573.66 |
| 溶解度 | DMSO : ≥ 40 mg/mL (69.73 mM);Water : 6.67 mg/mL (11.63 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7432 mL | 8.716 mL | 17.4319 mL |
| 5 mM | 348.6 μL | 1.7432 mL | 3.4864 mL |
| 10 mM | 174.3 μL | 871.6 μL | 1.7432 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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2.
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