Rufloxacin HCl
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MedKoo CAT#: 561626

CAS#: 106017-08-7

Description: Rufloxacin HCl is a quinolone antibiotic and antibacterial. It inhibits B-cell differentiation in human mononuclear cells and acts as an inhibitor of Topo.


Chemical Structure

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Rufloxacin HCl
CAS# 106017-08-7

Theoretical Analysis

MedKoo Cat#: 561626
Name: Rufloxacin HCl
CAS#: 106017-08-7
Chemical Formula: C17H19ClFN3O3S
Exact Mass: 0.00
Molecular Weight: 399.860
Elemental Analysis: C, 51.06; H, 4.79; Cl, 8.87; F, 4.75; N, 10.51; O, 12.00; S, 8.02

Price and Availability

Size Price Availability Quantity
25mg USD 205
50mg USD 340
100mg USD 525
250mg USD 750
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Synonym: Rufloxacin HCl; Rufloxacin Hydrochloride; MF 934; Ruflox; Monos; Qari; Tebraxin; Uroflox; Uroclar;

IUPAC/Chemical Name: 7-Fluoro-6-(4-methylpiperazin-1-yl)-10-oxo-4-thia-1-azatricyclo[7.3.1.05,13]trideca-5(13),6,8,11-tetraene-11-carboxylic acid hydrochloride

InChi Key: LPQOADBMXVRBNX-UHFFFAOYSA-N

InChi Code: InChI=1S/C17H18FN3O3S.ClH/c1-19-2-4-20(5-3-19)14-12(18)8-10-13-16(14)25-7-6-21(13)9-11(15(10)22)17(23)24;/h8-9H,2-7H2,1H3,(H,23,24);1H

SMILES Code: O=C(C1=CN2CCSC3=C2C(C1=O)=CC(F)=C3N4CCN(C)CC4)O.[H]Cl

Appearance: A crystalline solid

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO and water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Biological target: Rufloxacin is active against S. aureus, E. coli, P. aeruginosa, P. morganii, K. pneumoniae, and E. cloacae in vitro (MICs = 0.78, 0.78, 12.5, 1.56, <0.39, and <0.39 μg/ml, respectively). Rufloxacin inhibits M. luteus DNA gyrase with an IC50 value of 1.5 mM and inhibits DNA synthesis in S. aureus, E. coli, P. aeruginosa, K. pneumoniae, and E. cloacae (IC50s = 0.93, 1.03, 38.8, 0.55, and 0.66 μg/ml, respectively).
In vitro activity: Rufloxacin significantly inhibited hOCT1-mediated uptake under initial test conditions but did not inhibit hOCT2. Reference: Antimicrob Agents Chemother. 2013 Jun;57(6):2705-11. https://pubmed.ncbi.nlm.nih.gov/23545524/
In vivo activity: Rufloxacin is very effective on both mouse strains, but can completely eradicate the salmonellae from livers and spleens when given early in the infection of CBA resistant mice. Reference: J Chemother. 1992 Dec;4(6):353-7. https://pubmed.ncbi.nlm.nih.gov/1337552/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 0.1 0.21
Water 2.0 5.00

Preparing Stock Solutions

The following data is based on the product molecular weight 399.86 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Mulgaonkar A, Venitz J, Gründemann D, Sweet DH. Human organic cation transporters 1 (SLC22A1), 2 (SLC22A2), and 3 (SLC22A3) as disposition pathways for fluoroquinolone antimicrobials. Antimicrob Agents Chemother. 2013 Jun;57(6):2705-11. doi: 10.1128/AAC.02289-12. Epub 2013 Apr 1. PMID: 23545524; PMCID: PMC3716151. 2. Pessina A, Gribaldo L, Mineo E, Neri MG. In vitro short-term and long-term cytotoxicity of fluoroquinolones on murine cell lines. Indian J Exp Biol. 1994 Feb;32(2):113-8. PMID: 8045610. 3. Cuffini AM, Tullio V, Allocco A, Paizis G, De Leo C, Carlone NA. Effect of rufloxacin upon non-specific immune defences: in-vitro, ex-vivo and in-vivo results. J Antimicrob Chemother. 1994 Oct;34(4):545-53. doi: 10.1093/jac/34.4.545. PMID: 7868406. 4. Bonina L, Carbone M, Mastroeni P, Costa GB, Mastroeni P. Effects of rufloxacin in Salmonella typhimurium infection in mice. J Chemother. 1992 Dec;4(6):353-7. doi: 10.1080/1120009x.1992.11739191. PMID: 1337552.
In vitro protocol: 1. Mulgaonkar A, Venitz J, Gründemann D, Sweet DH. Human organic cation transporters 1 (SLC22A1), 2 (SLC22A2), and 3 (SLC22A3) as disposition pathways for fluoroquinolone antimicrobials. Antimicrob Agents Chemother. 2013 Jun;57(6):2705-11. doi: 10.1128/AAC.02289-12. Epub 2013 Apr 1. PMID: 23545524; PMCID: PMC3716151. 2. Pessina A, Gribaldo L, Mineo E, Neri MG. In vitro short-term and long-term cytotoxicity of fluoroquinolones on murine cell lines. Indian J Exp Biol. 1994 Feb;32(2):113-8. PMID: 8045610.
In vivo protocol: 1. Cuffini AM, Tullio V, Allocco A, Paizis G, De Leo C, Carlone NA. Effect of rufloxacin upon non-specific immune defences: in-vitro, ex-vivo and in-vivo results. J Antimicrob Chemother. 1994 Oct;34(4):545-53. doi: 10.1093/jac/34.4.545. PMID: 7868406. 2. Bonina L, Carbone M, Mastroeni P, Costa GB, Mastroeni P. Effects of rufloxacin in Salmonella typhimurium infection in mice. J Chemother. 1992 Dec;4(6):353-7. doi: 10.1080/1120009x.1992.11739191. PMID: 1337552.

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1. Piddock, L.J.V., Panchal, S., and Norte, V. Comparison of the mechanism of action and resistance of two new fluoroquinolones, rufloxacin and MF961 with those of ofloxacin and fleroxacin in Gram-negative and Gram-positive bacteria. J. Antimicrob. Chemother. 31(6), 855-863 (1993).

2. Cecchetti, V., Fravolini, A., Fringuelli, R., et al. Quinolonecarboxylic acids. 2. Synthesis and antibacterial evaluation of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids. J. Med. Chem. 30(3), 465-473 (1987).

3. Fabbri, S., Broggini, M., Pagella, P., et al. The inhibition of supercoiling activity of DNA gyrase from Micrococcus luteus caused by rufloxacin (MF 934) and MF 961. J. Antimicrob. Chemother. 27(5), 687-689 (1991).

4. Bonina, L., Carbone, M., Mastroeni, P., et al. Effects of rufloxacin in Salmonella typhimurium infection in mice. J. Chemother. 4(6), 353-357 (1992).