[CAS NO. ]  MifamurtideTFA

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PRODUCTS SPECIFICATIONS

Store
Catalog
HY-13682C
Brand
MCE
CAS
-

DESCRIPTION

Overview

MDL-
Molecular Weight1351.52
Molecular FormulaC61H110F3N6O21P
SMILESCCCCCCCCCCCCCCCC(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](NC(C)=O)C=O)C)=O)C)=O)C(N)=O)=O)C)=O)(O)=O)=O.OC(C(F)(F)F)=O

For research use only. We do not sell to patients.

Summary

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] .


IC50 & Target

NOD2


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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


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] .

MCE 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

NCT Number Sponsor Condition Start Date Phase
NCT03643133 UNICANCER
Osteosarcoma
October 23, 2018 Phase 2
NCT02441309 University of Oxford|Millennium: The Takeda Oncology Company|National Institute for Health Research, United Kingdom|Oxford University Hospitals NHS Trust|European Commission
Osteosarcoma
October 2014 Phase 2
NCT00631631 Millennium Pharmaceuticals, Inc.
Osteosarcoma
January 2008

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

4°C, sealed storage, away from moisture

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


Solvent & Solubility

In Vitro:

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

Preparing
Stock Solutions
Concentration Solvent Mass 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
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

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

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

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

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

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

* All of the co-solvents are available by MCE.