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MedKoo Cat#: 329413 | Name: Pazufloxacin Mesylate
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Pazufloxacin Mesylate, also known as Pazucross and T-3762, is a quinolone antibacterial agent used for the intravenous therapy of several infections. Pazufloxacin mesilate could induce the aggregation of glucose-reduced gold nanoparticles (AuNPs).

Chemical Structure

Pazufloxacin Mesylate
Pazufloxacin Mesylate
CAS#163680-77-1 (mesylate)

Theoretical Analysis

MedKoo Cat#: 329413

Name: Pazufloxacin Mesylate

CAS#: 163680-77-1 (mesylate)

Chemical Formula: C17H19FN2O7S

Exact Mass: 0.0000

Molecular Weight: 414.40

Elemental Analysis: C, 49.27; H, 4.62; F, 4.58; N, 6.76; O, 27.03; S, 7.74

Price and Availability

Size Price Availability Quantity
1g USD 250.00 2 weeks
5g USD 450.00 2 weeks
10g USD 650.00 2 weeks
25g USD 950.00 2 Weeks
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Related CAS #
163680-77-1 (mesylate) 127045-41-4 (free base)
Synonym
Pazufloxacin Mesylate; Pazucross; Pasil; T-3762; T 3762; T3762
IUPAC/Chemical Name
(S)-10-(1-aminocyclopropyl)-9-fluoro-3-methyl-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid compound with methanesulfonic acid (1:1)
InChi Key
UDHGFPATQWQARM-FJXQXJEOSA-N
InChi Code
InChI=1S/C16H15FN2O4.CH4O3S/c1-7-6-23-14-11(16(18)2-3-16)10(17)4-8-12(14)19(7)5-9(13(8)20)15(21)22;1-5(2,3)4/h4-5,7H,2-3,6,18H2,1H3,(H,21,22);1H3,(H,2,3,4)/t7-;/m0./s1
SMILES Code
O=C(C(C1=O)=CN2[C@@H](C)COC3=C(C4(N)CC4)C(F)=CC1=C23)O.CS(=O)(O)=O
Appearance
Solid powder
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
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
Related CAS# 127045-41-4 (Pazufloxacin ) 163680-77-1 (Pazufloxacin Mesylate)
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Pazufloxacin (T-3761) mesylate is a fluoroquinolone antibiotic.
In vitro activity:
The MICs of T-3761 against 90% of the streptococci and enterococci tested were 3.13 to 100 micrograms/ml. Its activity was equal to or 2- or 4-fold greater than those of norfloxacin and fleroxacin, equal to or 2- or 4-fold less than those of ofloxacin and ciprofloxacin, and 4- to 16-fold less than that of tosufloxacin. The activity of T-3761 against gram-negative bacteria was usually fourfold greater than those of norfloxacin, ofloxacin, and fleroxacin. Reference: Antimicrob Agents Chemother. 1992 Oct;36(10):2293-303. https://pubmed.ncbi.nlm.nih.gov/1332594/
In vivo activity:
When administered orally, T-3761 showed good efficacy in mice against systemic, pulmonary, and urinary tract infections with gram-positive and gram-negative bacteria, including quinolone-resistant Serratia marcescens and Pseudomonas aeruginosa. The in vivo activity of T-3761 was comparable to or greater than those of ofloxacin, ciprofloxacin, norfloxacin, and tosufloxacin against most infection models in mice. The activities of T-3761 were lower than those of tosufloxacin against gram-positive bacterial systemic and pulmonary infections in mice but not against infections with methicillin-resistant Staphylococcus aureus. The activities of T-3761 against systemic quinolone-resistant Serratia marcescens and Pseudomonas aeruginosa infections in mice were 2- to 14-fold greater than those of the reference agents. Reference: Antimicrob Agents Chemother. 1993 Mar;37(3):384-92. https://pubmed.ncbi.nlm.nih.gov/8460909/
Solvent mg/mL mM
Solubility
DMF 20.0 48.26
DMSO 62.5 150.82
Ethanol 1.0 2.41
PBS (pH 7.2) 10.0 24.13
Water 100.0 241.31
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 414.40 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. Higa F, Akamine M, Haranaga S, Tohyama M, Shinzato T, Tateyama M, Koide M, Saito A, Fujita J. In vitro activity of pazufloxacin, tosufloxacin and other quinolones against Legionella species. J Antimicrob Chemother. 2005 Dec;56(6):1053-7. doi: 10.1093/jac/dki391. Epub 2005 Oct 31. PMID: 16260445. 2. Muratani T, Inoue M, Mitsuhashi S. In vitro activity of T-3761, a new fluoroquinolone. Antimicrob Agents Chemother. 1992 Oct;36(10):2293-303. doi: 10.1128/AAC.36.10.2293. PMID: 1332594; PMCID: PMC245492. 3. Umezaki Y, Matsumoto K, Ikawa K, Yokoyama Y, Enoki Y, Shigemi A, Watanabe E, Nakamura K, Ueno K, Terazono H, Morikawa N, Takeda Y. Concentration-Dependent Activity of Pazufloxacin against Pseudomonas aeruginosa: An In Vivo Pharmacokinetic/Pharmacodynamic Study. Antibiotics (Basel). 2022 Jul 21;11(7):982. doi: 10.3390/antibiotics11070982. PMID: 35884236; PMCID: PMC9312304. 4. Fukuoka Y, Ikeda Y, Yamashiro Y, Takahata M, Todo Y, Narita H. In vitro and in vivo antibacterial activities of T-3761, a new quinolone derivative. Antimicrob Agents Chemother. 1993 Mar;37(3):384-92. doi: 10.1128/AAC.37.3.384. PMID: 8460909; PMCID: PMC187681.
In vitro protocol:
1. Higa F, Akamine M, Haranaga S, Tohyama M, Shinzato T, Tateyama M, Koide M, Saito A, Fujita J. In vitro activity of pazufloxacin, tosufloxacin and other quinolones against Legionella species. J Antimicrob Chemother. 2005 Dec;56(6):1053-7. doi: 10.1093/jac/dki391. Epub 2005 Oct 31. PMID: 16260445. 2. Muratani T, Inoue M, Mitsuhashi S. In vitro activity of T-3761, a new fluoroquinolone. Antimicrob Agents Chemother. 1992 Oct;36(10):2293-303. doi: 10.1128/AAC.36.10.2293. PMID: 1332594; PMCID: PMC245492.
In vivo protocol:
1. Umezaki Y, Matsumoto K, Ikawa K, Yokoyama Y, Enoki Y, Shigemi A, Watanabe E, Nakamura K, Ueno K, Terazono H, Morikawa N, Takeda Y. Concentration-Dependent Activity of Pazufloxacin against Pseudomonas aeruginosa: An In Vivo Pharmacokinetic/Pharmacodynamic Study. Antibiotics (Basel). 2022 Jul 21;11(7):982. doi: 10.3390/antibiotics11070982. PMID: 35884236; PMCID: PMC9312304. 2. Fukuoka Y, Ikeda Y, Yamashiro Y, Takahata M, Todo Y, Narita H. In vitro and in vivo antibacterial activities of T-3761, a new quinolone derivative. Antimicrob Agents Chemother. 1993 Mar;37(3):384-92. doi: 10.1128/AAC.37.3.384. PMID: 8460909; PMCID: PMC187681.
1: Huang Q, Wei W, Wang L, Chen H, Li T, Zhu X, Wu Y. Synthesis of uniform Ag nanosponges and its SERS application. Spectrochim Acta A Mol Biomol Spectrosc. 2018 Aug 5;201:300-305. doi: 10.1016/j.saa.2018.05.019. Epub 2018 May 9. PMID: 29763823. 2: Khan AM, Rampal S, Sood NK. Effect of levofloxacin, pazufloxacin, enrofloxacin, and meloxicam on the immunolocalization of ABCG-2 transporter protein in rabbit retina. Environ Sci Pollut Res Int. 2018 Mar;25(9):8853-8860. doi: 10.1007/s11356-018-1216-y. Epub 2018 Jan 12. PMID: 29330817. 3: Kong S, Liao M, Gu Y, Li N, Wu P, Zhang T, He H. Colorimetric recognition of pazufloxacin mesilate based on the aggregation of gold nanoparticles. Spectrochim Acta A Mol Biomol Spectrosc. 2016 Mar 15;157:244-250. doi: 10.1016/j.saa.2016.01.013. Epub 2016 Jan 9. PMID: 26774816. 4: Khan AM, Rampal S. Effects of repeated oral administration of pazufloxacin mesylate and meloxicam on the antioxidant status in rabbits. J Am Assoc Lab Anim Sci. 2014 Jul;53(4):399-403. PMID: 25199097; PMCID: PMC4113241. 5: Cao X, Lian L, Li H, Wu Y, Lou D. A fluorescence probe based on biomolecule- stabilized gold nanoclusters for the detection of pazufloxacin mesilate. Anal Sci. 2014;30(8):817-22. doi: 10.2116/analsci.30.817. PMID: 25109644. 6: Jiang L, Liu T, He H, Pham-Huy LA, Li L, Pham-Huy C, Xiao D. Adsorption behavior of pazufloxacin mesilate on amino-functionalized carbon nanotubes. J Nanosci Nanotechnol. 2012 Sep;12(9):7271-9. doi: 10.1166/jnn.2012.6562. PMID: 23035463. 7: Lee J, Seong SJ, Lim MS, Park SM, Park J, Seo JJ, Lee HW, Yoon YR. Single- dose pharmacokinetics and dose proportionality of intravenous pazufloxacin mesilate in healthy Korean volunteers. Expert Opin Drug Metab Toxicol. 2012 Aug;8(8):921-8. doi: 10.1517/17425255.2012.688951. PMID: 22809012. 8: Abe N, Fukuda S, Nakamura A, Taguchi Y, Matsuo S. [Evaluation of target attainment rate of pazufloxacin mesilate using Monte Carlo simulation method]. Jpn J Antibiot. 2010 Aug;63(4):319-25. Japanese. PMID: 21298865. 9: Chen Q, Zeng Y, Kuang J, Li Y, Li X, Zheng Y, Hou H, Hou S. Quantification of aesculin in rabbit plasma and ocular tissues by high performance liquid chromatography using fluorescent detection: application to a pharmacokinetic study. J Pharm Biomed Anal. 2011 Apr 28;55(1):161-7. doi: 10.1016/j.jpba.2011.01.004. Epub 2011 Jan 19. PMID: 21295934. 10: Wang XG, Miao J, Liang DR, Yu Q, Liang MZ, Zhang SH. [Clinical pharmacokinetics/pharmacodynamics study on pazufloxacin methanesulphonate injection]. Sichuan Da Xue Xue Bao Yi Xue Ban. 2009 Jul;40(4):689-93. Chinese. PMID: 19764574. 11: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2009 Mar;31(2):107-46. PMID: 19455266. 12: Kodama Y, Hori S, Tominaga S, Ohwada A, Yoshimi K, Sekiya M, Yamazaki M, Mori T, Suzuki T, Fukuchi Y, Takahashi K. [Evaluation of clinical effectiveness of Pazufloxacin Mesilate in acute exacerbation of chronic respiratory diseases]. Nihon Kokyuki Gakkai Zasshi. 2008 Oct;46(10):781-7. Japanese. PMID: 19044026. 13: Lou S, Li W, Hu Q. Influence of cefoperazone and azithromycin on the pharmacokinetics of pazufloxacin in rats. Eur J Drug Metab Pharmacokinet. 2007 Oct-Dec;32(4):219-23. doi: 10.1007/BF03191007. PMID: 18348471. 14: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2007 Nov;29(9):625-55. PMID: 18193114. 15: Liu YF, Huang KL, Peng DM, Ding P, Li GY. Preparation and characterization of glutaraldehyde cross-linked O-carboxymethylchitosan microspheres for controlled delivery of pazufloxacin mesilate. Int J Biol Macromol. 2007 Jun 1;41(1):87-93. doi: 10.1016/j.ijbiomac.2007.01.003. Epub 2007 Jan 19. PMID: 17292465. 16: Hara I, Miura T, Yamanaka K, Tanaka K, Yamada Y, Fujisawa M. A case of Sweet's syndrome following septic pulmonary emboli after high-dose chemotherapy for advanced testicular cancer. Int J Urol. 2006 Apr;13(4):481-4. doi: 10.1111/j.1442-2042.2006.01332.x. PMID: 16734883. 17: Higa F, Shinzato T, Toyama M, Haranaga S, Furugen M, Tateyama M, Kawakami K, Saito A. Efficacy of pazufloxacin mesilate in Legionnaires' disease: a case report and in vitro study of the isolate. J Infect Chemother. 2005 Jun;11(3):164-8. doi: 10.1007/s10156-005-0381-3. PMID: 15990982. 18: Fukuda H, Morita Y, Shiotani N, Mizuo M, Komae N. [Effect of pazufloxacin mesilate, a new quinolone antibacterial agent, for intravenous use on QT interval]. Jpn J Antibiot. 2004 Aug;57(4):404-12. Japanese. PMID: 15535041. 19: Chen S, Ma H, Zhao H, Feng R, Jin L. Terbium-sensitized fluorescence method for the determination of pazufloxacin mesilate and its application. Anal Sci. 2004 Jul;20(7):1075-8. doi: 10.2116/analsci.20.1075. PMID: 15293405. 20: Minami S, Hattori R, Matsuda A. [Pharmacological properties and expected clinical role of an injectable new quinolone antibiotic, pazufloxacin mesilate]. Nihon Yakurigaku Zasshi. 2003 Aug;122(2):161-78. Japanese. doi: 10.1254/fpj.122.161. PMID: 12890902.

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