Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
Other Sizes |
|
Purity: ≥98%
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. In terms of clinical efficacy, oral sitafloxacin was noninferior to oral levofloxacin in the treatment of community-acquired pneumonia or an infectious exacerbation of chronic respiratory tract disease, noninferior to oral tosufloxacin in the treatment of community-acquired pneumonia, and noninferior to oral levofloxacin in the treatment of complicated urinary tract infections, according to the results of randomized, double-blind, multicentre, noninferiority trials. Noncomparative studies demonstrated the efficacy of oral sitafloxacin in otorhinolaryngological infections, urethritis in men, C. trachomatis-associated cervicitis in women and odontogenic infections.
ln Vitro |
At MICs of 0.03, 0.12, and 0.06 mg/L, respectively, ciprofloxacin (DU6859a) has antibacterial activity against strains of Streptococcus pneumoniae, the gyrA mutant SP39, and the parC mutant 1026523 wild-type strain [1]. For EG 00093 and EG 00218 strains, respectively, ciprofloxacin (DU6859a) had MICs of 0.03 and 0.03 mg/L, indicating its antibacterial efficacy against quinolone-sensitive Streptococcus pneumoniae strains [1]. The inhibitory concentrations of sitafloxacin (DU6859a) are 4.38 mg/L for DNA gyrase and 3.12 mg/L for topoisomerase IV (TopoIV) [1].
|
---|---|
ln Vivo |
The antibacterial drug ciprofloxacin (DU-6859a) (12.5–100 mg/kg; ig; once daily for 4 weeks; female BALB/c mice) functions. M. Without any indication of footpad swelling, ulcerans cells can be extracted from implanted footpads [2].
|
Animal Protocol |
Animal/Disease Models: BALB/c female mice [2]
Doses: 12.5, 25, 50 and 100 mg/kg Route of Administration: po (oral gavage); one time/day for 4 weeks Experimental Results: Inhibition of Mycobacterium ulcerans and Mycobacterium ulcerans Cell growth. |
References |
[1]. 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.
[2]. Dhople AM, et al. Activities of sitafloxacin (DU-6859a), either singly or in combination with rifampin, against Mycobacterium ulcerans infection in mice. J Chemother. 2003 Feb;15(1):47-52. |
Molecular Formula |
C19H18CLF2N3O3
|
---|---|
Molecular Weight |
409.8178
|
Exact Mass |
409.1005
|
CAS # |
127254-12-0
|
Related CAS # |
Sitafloxacin hydrate;163253-35-8;Sitafloxacin hydrochloride;346607-37-2;Sitafloxacin monohydrate;163253-37-0
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
O=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
|
InChi Key |
PNUZDKCDAWUEGK-CYZMBNFOSA-N
|
InChi Code |
InChI=1S/C19H18ClF2N3O3/c20-14-15-8(17(26)9(18(27)28)5-25(15)12-4-10(12)21)3-11(22)16(14)24-6-13(23)19(7-24)1-2-19/h3,5,10,12-13H,1-2,4,6-7,23H2,(H,27,28)/t10-,12+,13+/m0/s1 SMILES
|
Chemical Name |
7-((S)-7-amino-5-azaspiro[2.4]heptan-5-yl)-8-chloro-6-fluoro-1-((1R,2S)-2-fluorocyclopropyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
|
Synonyms |
Sitafloxacin; Gracevit; Sitafloxacin [INN]; DU 6859; DU-6859a; DU 6859A; 3GJC60U4Q8
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
---|---|
Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4401 mL | 12.2005 mL | 24.4010 mL | |
5 mM | 0.4880 mL | 2.4401 mL | 4.8802 mL | |
10 mM | 0.2440 mL | 1.2200 mL | 2.4401 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.