| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| ln Vitro |
Mangafodipir trisodium (40, 200, and 1000 μM) inhibits H2O2's effect on the viability of HGrC cells [3]. At 200 and 1000 μM, mangafodipir trisodium mitigates the effects of cisplatin-induced HGrC cell viability [3].
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| ln Vivo |
Mice treated with manfodipir trisodium (10 mg/kg; intraperitoneal injection, once) did not exhibit skin injury from paclitaxel or cisplatin [3].
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| Animal Protocol |
Animal/Disease Models: Female CD-1 (ICR) mice cisplatin and paclitaxel-induced ovarian injury [3]
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip) injection; 10 mg/kg, once Experimental Results: Reduce the loss of primordial follicles, Decrease in secondary follicles and increase in antral follicles. Prevent changes in primary follicles caused by cisplatin and paclitaxel. Reduces the increase in caspase-3 levels induced by cisplatin and paclitaxel. |
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Organophosphate metabolism primarily occurs through oxidation, esterase hydrolysis, and reactions with glutathione. Demethylation and glucuronidation may also occur. Oxidation of organophosphate pesticides can produce moderately toxic products. Generally, thiophosphates themselves are not directly toxic and require oxidative metabolism to be converted into proximal toxins. Products produced by glutathione transferase reactions are generally less toxic. Paraoxygenase (PON1) is a key enzyme in organophosphate metabolism. PON1 can inactivate certain organophosphates through hydrolysis. PON1 hydrolyzes active metabolites in various organophosphate pesticides and nerve agents such as soman, sarin, and VX. The existence of PON1 polymorphism leads to differences in the enzyme level and catalytic efficiency of this esterase, which in turn suggests that different individuals may be more susceptible to the toxic effects of organophosphate exposure. |
| Toxicity/Toxicokinetics |
Toxicity Summary
Manganese is a cytotoxic agent that impairs transport systems, enzyme activity, and receptor function. It primarily targets the central nervous system, particularly the globus pallidus of the basal ganglia. Manganese ions (Mn(II)) are thought to enhance the auto-oxidation or turnover of various intracellular catecholamines, leading to increased production of free radicals, reactive oxygen species, and other cytotoxic metabolites, while simultaneously depleting cellular antioxidant defense mechanisms, ultimately resulting in oxidative damage and selective destruction of dopaminergic neurons. In addition to dopamine, manganese is also thought to disrupt other neurotransmitters, such as gamma-aminobutyric acid (GABA) and glutamate. For oxidative damage to occur, manganese must first inhibit the activity of the antioxidant enzyme manganese superoxide dismutase. The neurotoxicity of Mn(II) is also related to its ability to substitute for Ca(II) under physiological conditions. It can enter mitochondria via calcium uniporters, inhibiting mitochondrial oxidative phosphorylation. It may also inhibit Ca(II) efflux, leading to impaired mitochondrial membrane integrity. Mn(II) has been shown to significantly inhibit the activity of mitochondrial aconitase, thereby altering amino acid metabolism and cellular iron homeostasis. (L228) |
| References |
[1]. Karlsson JOG, et al. Mangafodipir a Selective Cytoprotectant - with Special Reference to Oxaliplatin and Its Association to Chemotherapy-Induced Peripheral Neuropathy (CIPN). Transl Oncol. 2017 Aug;10(4):641-649.
[2]. Wang C. Mangafodipir trisodium (MnDPDP)-enhanced magnetic resonance imaging of the liver and pancreas. Acta Radiol Suppl. 1998;415:1-31. [3]. Qin Y, et al. Protective effects of mangafodipir against chemotherapy-induced ovarian damage in mice. Reprod Biol Endocrinol. 2018 Oct 27;16(1):106. |
| Additional Infomation |
Mangafodipir Trisodium is the trisodium salt of manganese fordespyr and possesses potential antioxidant and chemoprotective activity. It consists of manganese(II) ions chelated on fordespyr (dipyridine diphosphate, or DPDP), enabling it to scavenge oxygen free radicals such as superoxide anions, hydrogen peroxide, and hydroxyl radicals, potentially preventing damage to macromolecules like DNA from oxygen free radicals and minimizing the damage to normal tissues caused by oxygen free radical-related chemotherapy toxicity. However, this drug may enhance the generation of oxygen free radicals in chemotherapy-induced tumor cells, thereby enhancing chemotherapy-induced cytotoxicity; tumor cells have higher levels of reactive oxygen species than normal cells, thus having a lower threshold for oxygen free radical-mediated cytotoxicity. Manganese fordespyr has traditionally been used as an imaging agent in magnetic resonance imaging (MRI). Manganese fordespyr is an intravenously injected contrast agent used to enhance the contrast of liver MRI. It consists of two parts: paramagnetic manganese(II) ions and the chelating agent fordespyr (dipyridine diphosphate, DPDP). Normal liver tissue absorbs more manganese than abnormal or cancerous tissue. Manganese shortens the longitudinal relaxation time (T1), making normal tissue appear brighter in magnetic resonance imaging (MRI) images. This enhanced contrast makes lesions easier to identify. Acute intravenous toxicity studies in mice, rats, and dogs showed that manganese floccopil has low to moderate toxicity. Repeat-dose toxicity studies have been conducted in rats, cynomolgus monkeys, and dogs. The liver, and to a lesser extent the kidneys, are the target organs for toxicity.
Drug Indications This drug is for diagnostic use only. As a contrast agent for diagnostic magnetic resonance imaging (MRI) to detect liver lesions suspected of being caused by metastatic disease or hepatocellular carcinoma. As an adjunct to MRI, to help examine focal pancreatic lesions. |
| Molecular Formula |
C22H24N4O14P2-8.MN+2.3[NA+]
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|---|---|
| Molecular Weight |
754.299360000001
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| Exact Mass |
757.007
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| CAS # |
140678-14-4
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| Related CAS # |
Mangafodipir;155319-91-8
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| PubChem CID |
160036
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| Appearance |
Brown to reddish brown solid powder
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| Boiling Point |
1049.1ºC at 760 mmHg
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| Flash Point |
588.3ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
18
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
46
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| Complexity |
873
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1[O-][Mn+2]([N]2(C3)CC4=C5COP(O)(O)=O)([O-]C6=C(N=C7)C)([O-]C4=C(N=C5)C)([O-]C3=O)[N](CC6=C7COP([O-])(O)=O)(CC2)C1.[Na+].[Na+].[Na+]
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| InChi Key |
BENFPBJLMUIGGD-UHFFFAOYSA-I
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| InChi Code |
InChI=1S/C22H32N4O14P2.Mn.3Na/c1-13-21(31)17(15(5-23-13)11-39-41(33,34)35)7-25(9-19(27)28)3-4-26(10-20(29)30)8-18-16(12-40-42(36,37)38)6-24-14(2)22(18)32;;;;/h5-6,31-32H,3-4,7-12H2,1-2H3,(H,27,28)(H,29,30)(H2,33,34,35)(H2,36,37,38);;;;/q;+2;3*+1/p-5
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| Chemical Name |
trisodium;2-[2-[carboxylatomethyl-[[2-methyl-3-oxido-5-(phosphonatooxymethyl)pyridin-4-yl]methyl]amino]ethyl-[[2-methyl-3-oxido-5-(phosphonatooxymethyl)pyridin-4-yl]methyl]amino]acetate;hydron;manganese(2+)
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| 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
H2O : ~33.33 mg/mL (~44.01 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (132.04 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3257 mL | 6.6287 mL | 13.2573 mL | |
| 5 mM | 0.2651 mL | 1.3257 mL | 2.6515 mL | |
| 10 mM | 0.1326 mL | 0.6629 mL | 1.3257 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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