| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
Fosmidomycin sodium targets 1-deoxy-D-xylulose-5-phosphate reductoisomerase (DXR), also known as IspC. DXR is a key enzyme in the non-mevalonate (MEP) pathway for isoprenoid biosynthesis, which is essential in many bacteria and in the malaria parasite Plasmodium falciparum. By inhibiting DXR, fosmidomycin blocks the production of isoprenoids, leading to bacterial and parasite death.
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|---|---|
| ln Vitro |
Fosminomycin sodium salt is an antibiotic that is phosphonate-based[1][2], effective against both Gram-positive and Gram-negative bacteria[3].
In vitro, fosmidomycin is a potent inhibitor of DXR. It has an IC50 of 290-370 nM against P. falciparum. It is active against both Gram-negative and Gram-positive bacteria. Its activity against the malaria parasite makes it a valuable antimalarial agent. |
| ln Vivo |
It appeared that animals given intraperitoneal doses of fosminomycin exceeding 10 mg/kg were free of parasites. Following 5 mg/kg fosminomycin treatment, the parasitemia was less than 1%. When 20 mg/kg of oral fosminomycin was administered, the parasitemia was less than 1%, and the animals treated with the antibiotic were significantly free of parasites. Relapse was noted upon stopping treatment after four days. After eight days of receiving 30 mg/kg fosminomycin, mice were totally cured [3].
In vivo, fosmidomycin has been shown to be an effective and safe antimalarial drug. Treatment with fosmidomycin is well-tolerated and shows rapid parasite and fever clearance. Its activity against bacterial infections has also been demonstrated in animal models. |
| Enzyme Assay |
In vitro enzyme assays for fosmidomycin measure its inhibition of DXR activity. The compound is incubated with DXR, 1-deoxy-D-xylulose-5-phosphate, and NADPH. The decrease in NADPH absorbance is monitored spectrophotometrically.
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| Cell Assay |
In vitro cell-based assays for fosmidomycin involve determining its minimum inhibitory concentration (MIC) against bacterial strains and its IC50 against P. falciparum in culture. The compound's antiparasitic activity is assessed by measuring parasite growth inhibition.
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| Animal Protocol |
In vivo animal experiments for fosmidomycin have been conducted in mouse models of malaria and bacterial infection. Animals are infected with P. falciparum or bacteria and treated with the compound. Efficacy is measured by survival rates, parasite clearance, and reduction in bacterial load.
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| ADME/Pharmacokinetics |
Fosmidomycin sodium has a molecular formula of C4H9NNaO5P. It is a crystalline solid with a purity of ≥95%. It is soluble in water. It is typically stored under recommended conditions for research compounds.
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| Toxicity/Toxicokinetics |
Fosmidomycin sodium is for research use only and is not intended for human use. Its safety profile has been evaluated in preclinical studies. It has been shown to be well-tolerated in animal models. Standard safety precautions should be taken when handling.
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| References |
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| Additional Infomation |
Fosmidomycin sodium salt is a phosphonic acid.
Fosmidomycin sodium is a phosphonic acid antibiotic and antimalarial agent. It inhibits DXR, a key enzyme in the non-mevalonate pathway. It is active against bacteria and P. falciparum. It has been shown to be an effective and safe antimalarial drug. It is also known as fosmidomycin sodium salt. |
| Molecular Formula |
C4H9NNAO5P
|
|---|---|
| Molecular Weight |
205.0815
|
| Exact Mass |
205.011
|
| CAS # |
66508-37-0
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| Related CAS # |
66508-37-0 (sodium); 66508-53-0 (free);
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| PubChem CID |
5141362
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| Appearance |
White to light brown solid powder
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| Boiling Point |
463.7ºC at 760 mmHg
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| Melting Point |
189-191ºC
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| Flash Point |
234.3ºC
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| LogP |
0.347
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
12
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| Complexity |
177
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| Defined Atom Stereocenter Count |
0
|
| InChi Key |
ZZPUYRHMTGOTEU-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C4H10NO5P.Na/c6-4-5(7)2-1-3-11(8,9)10;/h4,7H,1-3H2,(H2,8,9,10);/q;+1/p-1
|
| Chemical Name |
sodium;3-[formyl(hydroxy)amino]propyl-hydroxyphosphinate
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| Synonyms |
FR 31564; FR-31564; Fosmidomycin sodium
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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 : ~25 mg/mL (~121.90 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (487.61 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 | 4.8761 mL | 24.3807 mL | 48.7615 mL | |
| 5 mM | 0.9752 mL | 4.8761 mL | 9.7523 mL | |
| 10 mM | 0.4876 mL | 2.4381 mL | 4.8761 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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