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Purity: ≥98%
Garenoxacin (formerly BMS284756; T-3811ME, BMS-284756; tradename: Geninax) is a newly developed and orally bioavailable quinolone-based antibiotic for the treatment of Gram-positive and Gram-negative bacterial infections. Measurement of the MIC and the mutant prevention concentration (MPC) revealed that garenoxacin was 20-fold more potent than ciprofloxacin for a variety of ciprofloxacin-susceptible isolates, some of which were resistant to methicillin. The MPC for 90% of the isolates (MPC(90)) was below published serum drug concentrations achieved with recommended doses of garenoxacin. These in vitro observations suggest that garenoxacin has a low propensity for selective enrichment of fluoroquinolone-resistant mutants among ciprofloxacin-susceptible isolates of S. aureus. For ciprofloxacin-resistant isolates, the MIC at which 90% of the isolates tested were inhibited was below serum drug concentrations while the MPC(90) was not. Thus, for these strains, garenoxacin concentrations are expected to fall inside the mutant selection window (between the MIC and the MPC) for much of the treatment time. As a result, garenoxacin is expected to selectively enrich mutants with even lower susceptibility.
| Targets |
Quinolone;Gyrase(IC50=1.25 μg/mL);TOPO IV(IC50=1.5-2.5 μg/mL)
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| ln Vitro |
Against tested strains, Garenoxacin (BMS284756) (0-8 days) inhibits mycoplasmas and ureaplasmas with MIC90s ≤0.25 μg/mL [1].
S. aureus wild type and mutants are inhibited by genoxacin (48 h) with MICs ranging from 0.0128 to 4.0 μg/mL[2]. Garenoxacin has an IC50 of 1.25 to 2.5 μg/mL for topoisomerase IV and 1.25 μg/mL for gyrase from S. aureus, respectively[2]. Garenoxacin has a low tendency to selectively enrich fluoroquinolone-resistant mutants from S. aureus isolates that are susceptible to ciprofloxacin[3]. |
| ln Vivo |
Against the wild-type strain and mutants carrying a single mutation in a mouse pneumonia model with S. pneumonia infection, geldanoxin (12.5–50 mg/kg; s.c.; once) exhibits remarkable efficacy[4].
When BALB/c female mice are exposed to experimental secondary pneumococcal pneumonia caused by S. pneumoniae D-979, the viable cell counts in the lungs are reduced and their survival is significantly prolonged when garenoxacin (10 and 30 mg/kg; p.o.; once) is administered[5]. |
| Cell Assay |
Cell Line: Ureaplasma spp., M. pneumonia, M. fermentans, and M. hominis.
Incubation Time: 48 hours for M. hominis, 24 hours for Ureaplasma spp., and 4–8 days for M. pneumonia Result: demonstrated inhibition against strains of M. pneumonia, M. fermentans, M. hominis, and Ureaplasma spp. with MIC90s of 0.031 μg/mL, ≤0.008 μg/mL, ≤0.008 μg/mL, and 0.25 μg/mL, respectively. |
| Animal Protocol |
Animal Model: Swiss mice with S. pneumonia infection[4].
Dosage: 12.5, 25 and 50 mg/kg Administration: Subcutaneous injection, once Result: Significantly improved the survival rate. |
| References |
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| Additional Infomation |
Garenoxacin is a quinolinemonocarboxylic acid that is 1,4-dihydroquinoline-3-carboxylic acid that is substituted by a cyclopropyl group at position 1, an oxo group at position 4, a (1R)-1-methyl-2,3-dihydro-1H-isoindol-5-yl group at position 7, and a difluoromethoxy group at position 8. It has a role as an antibacterial drug and a non-steroidal anti-inflammatory drug. It is a quinolone antibiotic, a quinolinemonocarboxylic acid, an organofluorine compound, a member of cyclopropanes, an aromatic ether and a member of isoindoles.
Garenoxacin, a quinolone antibiotic, is being investigated for the treatment of gram-positive and gram-negative bacterial infections. Drug Indication Investigated for use/treatment in bacterial infection. |
| Molecular Formula |
C23H20F2N2O4
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|---|---|
| Molecular Weight |
426.412713050842
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| Exact Mass |
426.139
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| Elemental Analysis |
C, 64.78; H, 4.73; F, 8.91; N, 6.57; O, 15.01
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| CAS # |
194804-75-6
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| Related CAS # |
Garenoxacin Mesylate hydrate;223652-90-2;Garenoxacin mesylate;223652-82-2
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| PubChem CID |
124093
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| Appearance |
Solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
581.5±50.0 °C at 760 mmHg
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| Melting Point |
226-227°; mp 234-235°
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| Flash Point |
305.5±30.1 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.631
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| LogP |
2.28
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
31
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| Complexity |
771
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O=C(C1=CN(C2CC2)C3=C(C=CC(C4=CC5=C([C@@H](C)NC5)C=C4)=C3OC(F)F)C1=O)O
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| InChi Key |
NJDRXTDGYFKORP-LLVKDONJSA-N
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| InChi Code |
InChI=1S/C23H20F2N2O4/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/h2,5-8,10-11,14,23,26H,3-4,9H2,1H3,(H,29,30)/t11-/m1/s1
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| 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
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| Synonyms |
BMS-284756; BMS 284756; BMS284756; tradename: Geninax.
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~2 mg/mL ( ~4.69 mM )
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| 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 | 2.3452 mL | 11.7258 mL | 23.4516 mL | |
| 5 mM | 0.4690 mL | 2.3452 mL | 4.6903 mL | |
| 10 mM | 0.2345 mL | 1.1726 mL | 2.3452 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.
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