| Size | Price | Stock | Qty |
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| 1mg |
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| 10mg | |||
| Other Sizes |
| Targets |
Mifamurtide targets NOD-like receptors (NLRs), specifically NOD2, an intracellular MDP sensor primarily expressed on monocytes, dendritic cells, and macrophages. It also acts as a ligand for TLR4. By activating these receptors, Mifamurtide triggers innate immune responses, leading to macrophage and monocyte activation and the release of pro-inflammatory cytokines such as IL-1, IL-6, and TNF-α.
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| 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].
In vitro, Mifamurtide activates macrophages and monocytes, increasing their tumoricidal activity and inducing the release of pro-inflammatory cytokines. It stimulates the innate immune system through NOD2 and TLR4 activation. The compound has been studied in various in vitro assays measuring cytokine production, macrophage activation, and antitumor activity. |
| 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].
In vivo, Mifamurtide is used for the treatment of high-grade, resectable, non-metastatic osteosarcoma that is grossly resectable and completely excised. It has been shown to improve overall survival in patients with osteosarcoma when used in combination with chemotherapy. The compound activates macrophages and monocytes to enhance antitumor immune responses. |
| Enzyme Assay |
In vitro cellular assays for Mifamurtide typically use human monocytes, macrophages, or dendritic cells. Cells are treated with Mifamurtide at various concentrations, and cytokine production (TNF-α, IL-1, IL-6, IL-12) is measured by ELISA or multiplex immunoassay. Macrophage activation markers (CD80, CD86, HLA-DR) are assessed by flow cytometry. NOD2 and TLR4 signaling is evaluated by measuring downstream signaling pathways.
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| Cell Assay |
In vitro receptor binding assays for NOD2 agonists typically use cells expressing NOD2. Cells are treated with Mifamurtide, and NOD2-mediated NF-κB activation is measured using reporter gene assays or by assessing downstream signaling (e.g., phosphorylation of RIPK2, IKK). TLR4 activation is assessed using similar approaches in TLR4-expressing cells.
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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. In vivo animal studies for antitumor efficacy typically use mouse models of osteosarcoma or other tumors. Animals are administered Mifamurtide intravenously at various doses. Tumor growth is monitored, and immune cell infiltration and activation are assessed by flow cytometry and immunohistochemistry. Survival is monitored as an endpoint. Combination studies with chemotherapy may also be performed. |
| ADME/Pharmacokinetics |
Mifamurtide is administered intravenously as a liposomal formulation. The liposomal delivery system enhances its pharmacokinetic properties and targeting to macrophages and monocytes. The compound is metabolized in the liver and eliminated via the kidneys. Detailed PK parameters are available from clinical studies.
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| Toxicity/Toxicokinetics |
Mifamurtide is generally well-tolerated at therapeutic doses. Common side effects may include infusion-related reactions such as chills, fever, and fatigue. Serious adverse effects are rare. The compound has been evaluated in clinical trials for safety and efficacy in osteosarcoma patients. Its safety profile is well-established for the approved indication.
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| References |
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| Additional Infomation |
Drug Indication
Mepaltan is indicated for the treatment of high-grade, resectable, non-metastatic osteosarcoma that is grossly resectable and completely excised. It is intended for use in combination with postoperative multidrug chemotherapy. Its safety and efficacy have been evaluated in studies in patients aged 2 to 30 years at initial diagnosis. Mifamurtide (L-MTP-PE) is a liposomal immunomodulator that activates macrophages and monocytes via NOD2 and TLR4. It is used for the treatment of high-grade, resectable, non-metastatic osteosarcoma. The compound enhances antitumor immune responses and improves overall survival in combination with chemotherapy. It is available for clinical use. |
| Molecular Formula |
C59H109N6O19P
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|---|---|
| Molecular Weight |
1237.50000
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| Exact Mass |
1236.748
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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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| PubChem CID |
23725094
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Index of Refraction |
1.530
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| LogP |
10.98
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
19
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| Rotatable Bond Count |
54
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| Heavy Atom Count |
85
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| Complexity |
1960
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| Defined Atom Stereocenter Count |
8
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| SMILES |
CCCCCCCCCCCCCCCC(=O)OCC(COP(=O)(O)OCCNC(=O)[C@H](C)NC(=O)CC[C@H](C(=O)N)NC(=O)[C@H](C)NC(=O)[C@@H](C)O[C@@H]1[C@H]([C@@H](O[C@@H](C1O)CO)O)NC(=O)C)OC(=O)CCCCCCCCCCCCCCC
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| InChi Key |
JMUHBNWAORSSBD-ZXSMYVEWSA-N
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| InChi Code |
InChI=1S/C59H109N6O19P/c1-7-9-11-13-15-17-19-21-23-25-27-29-31-33-50(69)79-40-46(83-51(70)34-32-30-28-26-24-22-20-18-16-14-12-10-8-2)41-81-85(77,78)80-38-37-61-56(73)42(3)62-49(68)36-35-47(55(60)72)65-57(74)43(4)63-58(75)44(5)82-54-52(64-45(6)67)59(76)84-48(39-66)53(54)71/h42-44,46-48,52-54,59,66,71,76H,7-41H2,1-6H3,(H2,60,72)(H,61,73)(H,62,68)(H,63,75)(H,64,67)(H,65,74)(H,77,78)/t42-,43-,44+,46?,47+,48+,52+,53?,54+,59+/m0/s1
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| Chemical Name |
[3-[2-[[(2S)-2-[[(4R)-4-[[(2S)-2-[[(2R)-2-[(2R,3R,4R,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxypropanoyl]amino]propanoyl]amino]-5-amino-5-oxopentanoyl]amino]propanoyl]amino]ethoxy-hydroxyphosphoryl]oxy-2-hexadecanoyloxypropyl] hexadecanoate
|
| HS Tariff Code |
2934.99.9001
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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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