Mifamurtide (MTP-PE), an analog of the muramyl dipeptide (MDP), is a nonspecific immunomodulator by stimulating the immune response activating macrophages and monocytes. Mifamurtide, an orphan drug, is a specific ligand of NOD2 used as an insulin sensitizer. Mifamurtide has the potential for osteosarcoma research.
性状
Solid
IC50 & Target[1][2]
NOD2
体外研究(In Vitro)
Mifamurtide (MTP-PE; 100 μM) induces a reduction of MG63 cells number when co-cultured with macrophages. Mifamurtide (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 increases the iron transporter DMT1 protein. L-mifamurtide (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. Mifamurtide 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.
体内研究(In Vivo)
Mifamurtide (MTP-PE; 1 mg/kg; i.v.; twice per week for 4 weeks) causes a trend of diminished spontaneous lung metastasis dissemination.
Mifamurtide (50 μg/mouse) improves glucose tolerance during endotoxemia in mice. Mifamurtide (equivalent to 20 μg MDP; 4 times per week for 5 weeks) improves glucose tolerance in HFD-fed mice without altering body mass. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
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]. 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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (80.81 mM; Need ultrasonic)配制储备液