Garenoxacin mesylate hydrate | CAS#223652-90-2 | antibiotic

MedKoo Cat#: 525152 | Name: Garenoxacin mesylate hydrate

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Description:

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

Garenoxacin mesylate hydrate is a novel oral des-fluoro quinolone with potent antimicrobial activity against common respiratory pathogens, including resistant strains and Gram-positive and Gram-negative bacterial infections.

Chemical Structure

Garenoxacin mesylate hydrate

CAS#223652-90-2 (mesylate hydrate)

Theoretical Analysis

MedKoo Cat#: 525152

Name: Garenoxacin mesylate hydrate

CAS#: 223652-90-2 (mesylate hydrate)

Chemical Formula: C24H26F2N2O8S

Exact Mass: 0.0000

Molecular Weight: 540.53

Elemental Analysis: C, 53.33; H, 4.85; F, 7.03; N, 5.18; O, 23.68; S, 5.93

Price and Availability

Size	Price	Availability
10mg	USD 350.00	2 Weeks
25mg	USD 650.00	2 Weeks
50mg	USD 950.00	2 Weeks
100mg	USD 1,450.00	2 Weeks

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Related CAS #

223652-82-2 (mesylate) 194804-75-6 (free base) 223652-90-2 (mesylate hydrate)

Synonym

Garenoxacin mesylate hydrate; Garenoxacin methanesulfonic acid hydrate; Garenoxacin mesilate hydrate; BMS284756; BMS 284756; BMS-284756; T-3811; T 3811; T3811;

IUPAC/Chemical Name

1-Cyclopropyl-8-(difluoromethoxy)-7-((1R)-1-methyl-2,3-dihydro-1H-isoindol-5-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid monomethanesulfonate monohydrate

InChi Key

IGTHEWGRXUAFKF-NVJADKKVSA-N

InChi Code

InChI=1S/C23H20F2N2O4.CH4O3S.H2O/c1-11-15-5-2-12(8-13(15)9-26-11)16-6-7-17-19(21(16)31-23(24)25)27(14-3-4-14)10-18(20(17)28)22(29)30;1-5(2,3)4;/h2,5-8,10-11,14,23,26H,3-4,9H2,1H3,(H,29,30);1H3,(H,2,3,4);1H2/t11-;;/m1../s1

SMILES Code

O=C(C1=CN(C2CC2)C3=C(C=CC(C4=CC5=C([C@@H](C)NC5)C=C4)=C3OC(F)F)C1=O)O.CS(=O)(O)=O.[H]O[H]

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

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Garenoxacin Mesylate hydrate (BMS284756 Mesylate hydrate) is a novel oral des-fluoro(6) quinolone with potent antimicrobial activity, against common respiratory pathogens, including resistant strains.

In vitro activity:

Table 1 indicates that garenoxacin was 4 to 16 times more active than levofloxacin against the S. aureus and VGS isolates used in this study. Reference: Antimicrob Agents Chemother. 2004 Jan;48(1):86-92. https://pubmed.ncbi.nlm.nih.gov/14693523/

In vivo activity:

Garenoxacin at 25 and 50 mg/kg was highly effective (survival rates, 85 to 100%) against the wild-type strain and mutants harboring a single mutation. TVA was as effective as garenoxacin against these strains. TVA at 200 mg/kg and garenoxacin at 50 mg/kg were ineffective against the mutant with the parC and gyrA double mutations and the mutant with the gyrA, parC, and parE triple mutations. Reference: Antimicrob Agents Chemother. 2004 Mar;48(3):765-73. https://pubmed.ncbi.nlm.nih.gov/14982762/

	Solvent	mg/mL	mM
Solubility
	DMSO	100.0	185.00
	Water	12.5	23.13

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 540.53 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.

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. Yamamoto K, Yanagihara K, Sugahara K, Imamura Y, Seki M, Izumikawa K, Kakeya H, Yamamoto Y, Hirakata Y, Kamihira S, Kohno S. In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms. Antimicrob Agents Chemother. 2009 Aug;53(8):3572-5. doi: 10.1128/AAC.00176-09. Epub 2009 May 18. PMID: 19451290; PMCID: PMC2715604. 2. Entenza JM, Vouillamoz J, Glauser MP, Moreillon P. Efficacy of garenoxacin in treatment of experimental endocarditis due to Staphylococcus aureus or viridans group streptococci. Antimicrob Agents Chemother. 2004 Jan;48(1):86-92. doi: 10.1128/AAC.48.1.86-92.2004. PMID: 14693523; PMCID: PMC310157. 3. Azoulay-Dupuis E, Bédos JP, Mohler J, Peytavin G, Isturiz R, Moine P, Rieux V, Cherbuliez C, Péchère JC, Fantin B, Köhler T. Activities of garenoxacin against quinolone-resistant Streptococcus pneumoniae strains in vitro and in a mouse pneumonia model. Antimicrob Agents Chemother. 2004 Mar;48(3):765-73. doi: 10.1128/AAC.48.3.765-773.2004. PMID: 14982762; PMCID: PMC353052.

In vitro protocol:

In vivo protocol:

1. Azoulay-Dupuis E, Bédos JP, Mohler J, Peytavin G, Isturiz R, Moine P, Rieux V, Cherbuliez C, Péchère JC, Fantin B, Köhler T. Activities of garenoxacin against quinolone-resistant Streptococcus pneumoniae strains in vitro and in a mouse pneumonia model. Antimicrob Agents Chemother. 2004 Mar;48(3):765-73. doi: 10.1128/AAC.48.3.765-773.2004. PMID: 14982762; PMCID: PMC353052.

1: Takagi H, Tanaka K, Tsuda H, Kobayashi H. Clinical studies of garenoxacin. Int J Antimicrob Agents. 2008 Dec;32(6):468-74. doi: 10.1016/j.ijantimicag.2008.06.032. Epub 2008 Sep 13. Review. PubMed PMID: 18790608.