| Size | Price | Stock | Qty |
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| 1mg |
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Mifamurtide is a liposomal formulation containing a muramyl dipeptide (MDP) analogue with potential immunomodulatory and antineoplastic activities.. Muramyl tripeptide phosphatidylethanolamine (MTP-PE), a analogue of the mycobacterial cell wall component MDP, activates both monocytes and macrophages. Activated macrophages secrete cytokines and induce the recruitment and activation of other immune cells, which may result in indirect tumoricidal effects. Liposomal encapsulation of MTP-PE prolongs its half-life and enhances tissue targeting. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).
| ln Vitro |
When co-cultured with macrophages, mifamurtide (MTP-PE; 100 µM) reduces the number of MG63 cells [3]. The M1 polarization marker iNOS and the M2 polarization marker CD206 mRNA, as well as pro- and anti-inflammatory cytokines (IL-1β, IL-6) and IL-4, IL-10), are increased by mifamurtide (100 µM). The iron transporter DMT1 protein is increased by mifamotide [3]. The two osteosarcoma cell lines, MOS-J and KHOS, do not exhibit any direct effects on the rate of proliferation of L-mifamotide alone (5, 5000 nM; 48 hours of action) either in vitro or in vivo [1]. Mifamotide is a non-specific immunomodulator that activates macrophages and monocytes to increase tumoricidal activity and release pro-inflammatory cytokines, such as interleukin (IL) and tumor necrosis factor (TNF)-a. -1, prostaglandin E2 (PGE2), IL-6, IL-8, IL-12, nitric oxide (NO), and PGD2[3].
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| ln Vivo |
There is a propensity for mifamotide (MTP-PE; 1 mg/kg; intravenously administered twice weekly for 4 weeks) to inhibit the spread of spontaneous pulmonary metastases [1]. In mice with endotoxemia, mifamotide (50 μg/mouse) enhances glucose tolerance. Without affecting body weight, mifamurtide (equal to 20 μg MDP) increases glucose tolerance in HFD-fed rats when administered four times a week for five weeks [2].
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| Animal Protocol |
Animal/Disease Models: C57BL/6, balb/c (Bagg ALBino) mouse with KHOS osteosarcoma cells [1]
Doses: 1 mg/kg Route of Administration: IV; twice weekly for 4 weeks Experimental Results: Results in xenogeneic (KHOS) and Trend toward diminished spread of spontaneous lung metastases in a syngeneic (MOS-J) model. |
| References |
[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]. Mifamurtide: CGP 19835, CGP 19835A, L-MTP-PE, liposomal MTP-PE, MLV 19835A, MTP-PE, muramyltripeptide phosphatidylethanolamine. Drugs R D, 2008. 9(2): p. 131-5. [3]. 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. [4]. 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. |
| Molecular Formula |
C59H109N6O19P
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|---|---|
| Molecular Weight |
1237.50000
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| CAS # |
83461-56-7
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| Related CAS # |
Mifamurtide sodium;90825-43-7;Mifamurtide TFA;Mifamurtide sodium hydrate;838853-48-8
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| SMILES |
CCCCCCCCCCCCCCCC(OC[C@@H](OC(CCCCCCCCCCCCCCC)=O)COP(OCCNC([C@@H](NC(CC[C@@H](NC([C@@H](NC([C@H](O[C@]([C@H](O)[C@H](O)CO)([H])[C@H](C=O)NC(C)=O)C)=O)C)=O)C(N)=O)=O)C)=O)(O)=O)=O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~80.81 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.02 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (2.02 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.02 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.8081 mL | 4.0404 mL | 8.0808 mL | |
| 5 mM | 0.1616 mL | 0.8081 mL | 1.6162 mL | |
| 10 mM | 0.0808 mL | 0.4040 mL | 0.8081 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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