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| 10mg |
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| 25mg |
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Cefiderocol (S-649266; GSK-2696266D; S-649266D; trade name Fetroja) is an injectable siderophore cephalosporin antibiotic that has a catechol moiety on the 3-position of the side chain and was under clinical trials by Shionogi. It exhibits potent in vitro activity against the non-fermenting Gram- bacteria such as Acinetobacter baumannii, Pseudomonas aeruginosa and Stenotrophomonas maltophilia. As of Nov 14, 2019, Cefiderocol has gained FDA approval to treat patients with complicated UTI-urinary tract infections who have no other options available. It is indicated for the treatment of multi-drug-resistant Gram- bacteria such as Pseudomonas aeruginosa.
| Targets |
β-lactam
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|---|---|
| ln Vitro |
Cefiderocol (S-649266) is a new parenteral siderophore cephalosporin conjugated with a catechol moiety. It has a strong antibacterial activity against a variety of aerobic Gram-negative bacterial species, including nonfermenting bacteria like Pseudomonas aeruginosa and Acinetobacter baumannii and carbapenem-resistant strains of Enterobacteriaceae. Cefiderocol primarily binds to nonfermenting bacteria, such as GR20263, and PBP3 of the Enterobacteriaceae family. Cefiderocol MICs can rise 16-fold when the iron transporters PiuA in P. aeruginosa or CirA and Fiu in Escherichia coli are deficient, indicating that these iron transporters aid in cefiderocol's penetration through the outer membrane.Cefiderocol activity is not significantly affected by the overproduction of the efflux pump MexA-MexB-OprM in P. aeruginosa or the deficiency of OmpK35/36 in Klebsiella pneumoniae[1].
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| Cell Assay |
Except in situations where MICs under particular circumstances must be determined, iron-depleted cation-adjusted Mueller-Hinton broth (ID-CAMHB) is prepared for the purpose of determining the cefiderocol MIC. Cefiderocol's quality control minimum inhibitory concentration (MIC) ranges for E. Coli ATCC 25922 and P. aeruginosa ATCC 27853 are 0.06 to 0.5 μg/mL. Brusecella agar supplemented with hemin, vitamin K1, and laked sheep blood is used for anaerobic bacteria[1].
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| References |
| Molecular Formula |
C30H34CLN7O10S2
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|---|---|
| Molecular Weight |
752.21
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| Exact Mass |
751.1497
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| Elemental Analysis |
C, 47.90; H, 4.56; Cl, 4.71; N, 13.03; O, 21.27; S, 8.52
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| CAS # |
1225208-94-5
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| Related CAS # |
1883830-01-0 (ditosylate hydrate);1225208-94-5;2009350-94-9 (sulfate tosylate 3:1:4);2135543-94-9 (sulfate tosylate hydrate 3:1:4:1);
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| Appearance |
Solid powder
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| SMILES |
OC(C(O)=C1Cl)=CC=C1C(NCC[N+]2(CCCC2)CC3=C(C([O-])=O)N4C([C@H]([C@]4(SC3)[H])NC(/C(C5=CSC(N)=N5)=N\OC(C(O)=O)(C)C)=O)=O)=O
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| InChi Key |
DBPPRLRVDVJOCL-FQRUVTKNSA-N
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| InChi Code |
InChI=1S/C30H34ClN7O10S2/c1-30(2,28(46)47)48-36-19(16-13-50-29(32)34-16)24(42)35-20-25(43)37-21(27(44)45)14(12-49-26(20)37)11-38(8-3-4-9-38)10-7-33-23(41)15-5-6-17(39)22(40)18(15)31/h5-6,13,20,26H,3-4,7-12H2,1-2H3,(H7-,32,33,34,35,36,39,40,41,42,44,45,46,47)/t20-,26-/m1/s1
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| Chemical Name |
(6R,7R)-7-[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-{[(2-carboxypropan-2-yl)oxy]imino}acetamido]-3-({1-[2-(2-chloro-3,4-dihydroxybenzamido)ethyl]pyrrolidin-1-ium-1-yl}methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate
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| Synonyms |
S-649266; S 649266; S649266; GSK2696266D; GSK-2696266D; GSK 2696266D; S-649266D; S 649266D; S649266D; Cefiderocol; Fetroja.
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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: (1). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. (2). This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| 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 : ≥ 125 mg/mL (~166.18 mM)
H2O : ~1.06 mg/mL (~1.41 mM) Ethanol : < 1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (3.66 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 27.5 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: ≥ 2.75 mg/mL (3.66 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 27.5 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: ≥ 2.75 mg/mL (3.66 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.75 mg/mL (3.66 mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3294 mL | 6.6471 mL | 13.2942 mL | |
| 5 mM | 0.2659 mL | 1.3294 mL | 2.6588 mL | |
| 10 mM | 0.1329 mL | 0.6647 mL | 1.3294 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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