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。
| 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 ofNOD2used as aninsulinsensitizer. Mifamurtide TFA has the potential for osteosarcoma research[1][2][3]. |
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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].
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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].
| 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. |
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| 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℃) 配制储备液 | 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 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。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 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本网站选购。
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