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Sitafloxacin (DU-6859a)

This product is for research use only, not for human use. We do not sell to patients.

Sitafloxacin (DU-6859a)
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Cat #: V21049 CAS #: 127254-12-0 Purity ≥ 98%

Description: Sitafloxacin Hydrate (DU-6859a), a new-generation, broad-spectrum and orally bioavailable fluoroquinolone class of antibiotic, is highly active against many Gram-positive, Gram-negative and anaerobic clinical isolates, including strains resistant to other fluoroquinolones, was recently approved in Japan for the treatment of respiratory and urinary tract infections.

References: Okumura R, et al. Dual-targeting properties of the 3-aminopyrrolidyl quinolones, DC-159a and sitafloxacin, against DNA gyrase and topoisomerase IV: contribution to reducing in vitro emergence of quinolone-resistant Streptococcus pneumoniae. J Antimicrob Chemother. 2008 Jul;62(1):98-104.

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Molecular Weight (MW)409.81
Molecular FormulaC19H18ClF2N3O3
CAS No.127254-12-0
SMILES CodeO=C(C1=CN([C@H]2[C@@H](F)C2)C3=C(C=C(F)C(N(C[C@H]4N)CC54CC5)=C3Cl)C1=O)O.O=C(C6=CN([C@H]7[C@@H](F)C7)C8=C(C=C(F)C(N(C[C@H]9N)CC%109CC%10)=C8Cl)C6=O)O.[H]O[H].[H]O[H].[H]O[H]
SynonymsSitafloxacin hydrate; Sitafloxacin anhydrous; Sitafloxacin; DU 6859; DU-6859; DU6859; DU 6859A; DU-6859A; DU6859A; Trade name: Gracevit.
ProtocolIn VitroSitafloxacin (DU6859a) shows inhibition for DNA gyrase and topoisomerase IV (TopoIV) with >IC50s of 4.38, 3.12 mg/L, respectively. Sitafloxacin (DU6859a) shows antibacterial activities for quinolone-susceptible strains of streptococcus pneumoniae with MIC of 0.03, 0.03 mg/L for EG 00093 and EG 00218 strain, respectively. Sitafloxacin (DU6859a) shows antibacterial activities with MIC of 0.03, 0.12, 0.06 mg/L for wild-type ATCC 49619, gyrA mutant SP39, parC mutant 1026523 streptococcus pneumoniae stran, respectively.
In VivoSitafloxacin (DU-6859a) (12.5-100 mg/kg; i.g.; daily for 4 weeks; BALB/c female mice) has antibacterial activity. M. ulcerans cells could be isolated from the inoculated footpads and there was no evidence of footpad swelling.
Animal modelBALB/c female mice
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.4402 mL12.2008 mL24.4016 mL48.8031 mL
5mM0.4880 mL2.4402 mL4.8803 mL9.7606 mL
10mM0.2440 mL1.2201 mL2.4402 mL4.8803 mL
20mM0.1220 mL0.6100 mL1.2201 mL2.4402 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid 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 master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (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.