Mifamurtide TFA(Synonyms: 米伐木肽 TFA 盐; MTP-PE TFA; L-MTP-PE TFA; CGP 19835 TFA)

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Mifamurtide TFA (Synonyms: 米伐木肽 TFA 盐; MTP-PE TFA; L-MTP-PE TFA; CGP 19835 TFA) 纯度: ≥98.0%

Mifamurtide TFA (MTP-PE TFA) 是穆拉基二肽 (MDP) 的类似物,一种非特异性免疫调节剂,通过刺激激活巨噬细胞和单核细胞的免疫应答而发挥作用。Mifamurtide TFA 是一种孤儿药,是 NOD2 的特异性配体,用作胰岛素增敏剂。Mifamurtide TFA 具有用于骨肉瘤研究的潜力。

Mifamurtide TFA(Synonyms: 米伐木肽 TFA 盐; MTP-PE TFA; L-MTP-PE TFA; CGP 19835 TFA)

Mifamurtide TFA Chemical Structure

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Mifamurtide TFA 相关产品

相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus

生物活性

Mifamurtide TFA (MTP-PE TFA), an analog of the muramyl dipeptide (MDP), is a nonspecific immunomodulator by stimulating the immune response activating macrophages and monocytes. Mifamurtide TFA, an orphan drug, is a specific ligand of NOD2 used as an insulin sensitizer. Mifamurtide TFA has the potential for osteosarcoma research[1][2][3].

体外研究
(In Vitro)

Mifamurtide TFA (MTP-PE TFA; 100 µM) induces a reduction of MG63 cells number when co-cultured with macrophages[3].
Mifamurtide TFA (100 µM) increases both the M1 polarization marker iNOS and the M2 polarization marker CD206 mRNAs; both pro-inflammatory (IL-1β, IL-6) and anti-inflammatory (IL-4, IL-10) cytokines. Mifamurtide TFA increases the iron transporter DMT1 protein[3].
L-mifamurtide TFA (5, 5000 nM; for 48 hours) alone has no direct effect on the proliferation rate of the two osteosarcoma cell lines MOS-J and KHOS in vitro or in vivo[1].
Mifamurtide TFA acts as a nonspecific immunomodulator by activating macrophages and monocytes related to the upregulation of tumoricidal activity and secretion of pro-inflammatory cytokines including tumor necrosis factor (TNF)-a, interleukin (IL)-1, IL-6, IL-8, IL-12, nitric oxide (NO), prostaglandin E2 (PGE2) and PGD2[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Mifamurtide TFA (MTP-PE TFA; 1 mg/kg; i.v.; twice per week for 4 weeks) causes a trend of diminished spontaneous lung metastasis dissemination[1].
Mifamurtide TFA (50 μg/mouse) improves glucose tolerance during endotoxemia in mice. Mifamurtide TFA (equivalent to 20 μg MDP; 4 times per week for 5 weeks) improves glucose tolerance in HFD-fed mice without altering body mass[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6, BALB/c mice with KHOS osteosarcoma cells[1]
Dosage: 1 mg/kg
Administration: IV; twice per week for 4 weeks
Result: Caused a trend of diminished spontaneous lung metastasis dissemination in xenogeneic (KHOS) and syngeneic (MOS-J) models.

Clinical Trial

分子量

1351.52

Formula

C61H110F3N6O21P

中文名称

米伐木肽 TFA 盐;米法莫肽 TFA 盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 25 mg/mL (18.50 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.7399 mL 3.6995 mL 7.3991 mL
5 mM 0.1480 mL 0.7399 mL 1.4798 mL
10 mM 0.0740 mL 0.3700 mL 0.7399 mL

*

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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (1.85 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.85 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (1.85 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (1.85 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (1.85 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (1.85 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Kevin Biteau, et al. L-MTP-PE and zoledronic acid combination in osteosarcoma: preclinical evidence of positive therapeutic combination for clinical transfer. Am J Cancer Res. 2016 Feb 15;6(3):677-89.

    [2]. Joseph F Cavallari, et al. Muramyl Dipeptide-Based Postbiotics Mitigate Obesity-Induced Insulin Resistance via IRF4. Cell Metab. 2017 May 2;25(5):1063-1074.e3.

    [3]. Francesca Punzo, et al. Mifamurtide and TAM-like macrophages: effect on proliferation, migration and differentiation of osteosarcoma cells. Oncotarget. 2020 Feb 18;11(7):687-698.

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