| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
The primary molecular targets of Grepafloxacin hydrochloride are bacterial DNA gyrase and topoisomerase IV. It inhibits these enzymes by stabilizing the enzyme-DNA cleavage complex, preventing DNA replication and transcription. In Streptococcus pneumoniae, Grepafloxacin acts preferentially through gyrase, while in other bacteria it may target both enzymes. The C-5 group of Grepafloxacin contributes to its target specificity.
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| ln Vitro |
The antibiotic ciprofloxacin (OPC-17116; 0-1 mg/L; 14-21 d) hydrochloride exhibits a minimum inhibitory concentration (MIC) of < 0.006 mg/L for the strain of E. coli [1]. Against mycobacteria in macrophages, grepafloxacin (0–1 mg/L; 3 h) hydrochloride exhibits antibacterial action, with a minimum inhibitory concentration (MIC) of 0.5 mg/L for M. avium[1]. The in vivo efficacy of grepafloxacin hydrochloride against experimental systemic infections caused by both Gram-positive and -negative bacteria is high, and it demonstrates strong in vitro antibacterial action against Gram-positive bacteria such Streptococcus pneumoniae[4].
In vitro, Grepafloxacin hydrochloride exhibits potent activity against community-acquired respiratory pathogens including Streptococcus pneumoniae. It has high tissue penetration and a promising pharmacodynamic profile. Grepafloxacin acts preferentially through gyrase in Streptococcus pneumoniae, with the C-5 group playing a role in target specificity. It demonstrates broad-spectrum antimicrobial activity. |
| ln Vivo |
In terms of phototoxicity, grepafloxacin hydrochloride (OPC-17116; 200 mg/kg; po; Balb/c mice) exhibits a good safety profile[2]. In models of intravenous (IV) and intranasal (IN) Mycobacterium avium infection, grepafloxacin (25–200 mg/kg; po; 5 days/week for 4 weeks; female C57BL6/J-Lyst bg-J/ mice/beige mice) hydrochloride has moderate activities[3].
In vivo, Grepafloxacin hydrochloride is an orally active fluoroquinolone antibiotic. It achieves high tissue concentrations and is effective against respiratory tract infections. The compound was clinically used for chronic bronchitis and other bacterial infections before being withdrawn from the market. Specific pharmacokinetic parameters and efficacy data are documented in clinical literature. |
| Enzyme Assay |
Non-cell-based assays for Grepafloxacin hydrochloride use purified bacterial DNA gyrase and topoisomerase IV. The assay measures ATP-dependent supercoiling of relaxed plasmid DNA or decatenation of kinetoplast DNA. Grepafloxacin is added at varying concentrations, and IC50 values are determined from dose-response curves.
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| Cell Assay |
Cell-based assays for Grepafloxacin hydrochloride use bacterial cultures. MIC values are determined by broth microdilution in Mueller-Hinton broth against Streptococcus pneumoniae and other respiratory pathogens. Time-kill curves are performed at 1×, 2×, and 4× MIC.
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| Animal Protocol |
In vivo protocols for Grepafloxacin hydrochloride use rodent models of respiratory tract infection. Animals receive oral Grepafloxacin at doses determined by pharmacokinetic studies. Bacterial burden in lungs is quantified by colony counting. Serum and tissue drug concentrations are measured by HPLC. Clinical efficacy was evaluated in human trials for chronic bronchitis.
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| References |
[1]. Vacher S, et, al. Comparative antimycobacterial activities of ofloxacin, ciprofloxacin and grepafloxacin. J Antimicrob Chemother. 1999 Nov;44(5):647-52.
[2]. Owen K. Comparative grepafloxacin phototoxicity in mouse skin. J Antimicrob Chemother. 1998 Aug;42(2):261-4. [3]. Cynamon MH, et, al. The activity of grepafloxacin in two murine models of Mycobacterium avium infection. J Infect Chemother. 2004 Jun;10(3):185-8. [4]. Miyamoto H, et al. Synthesis and biological properties of substituted 1,4-dihydro-5-methyl-4-oxo-3-quinolinecarboxylic acids. Bioorg Med Chem. 1995;3(12):1699-1706. |
| Molecular Formula |
C19H23CLFN3O3
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|---|---|
| Molecular Weight |
395.86
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| Exact Mass |
395.141
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| CAS # |
161967-81-3
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| Related CAS # |
Grepafloxacin;119914-60-2
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| PubChem CID |
656829
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| Appearance |
Yellow to orange solid powder
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| Boiling Point |
626.7ºC at 760mmHg
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| Flash Point |
332.8ºC
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| Vapour Pressure |
1.43E-16mmHg at 25°C
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| LogP |
3.476
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| tPSA |
74.57
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
27
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| Complexity |
636
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.C1(N2C3C(=C(C)C(F)=C(N4CCNC(C)C4)C=3)C(=O)C(C(O)=O)=C2)CC1
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| InChi Key |
IEPMBYOIQGCVHO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H22FN3O3.ClH/c1-10-8-22(6-5-21-10)15-7-14-16(11(2)17(15)20)18(24)13(19(25)26)9-23(14)12-3-4-12/h7,9-10,12,21H,3-6,8H2,1-2H3,(H,25,26)1H
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| Chemical Name |
1-cyclopropyl-6-fluoro-5-methyl-7-(3-methylpiperazin-1-yl)-4-oxoquinoline-3-carboxylic acidhydrochloride
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| Synonyms |
OPC 17116 OPC-17116 OPC-17116Raxar
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
H2O : ≥ 13.33 mg/mL (~33.67 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 | 2.5261 mL | 12.6307 mL | 25.2615 mL | |
| 5 mM | 0.5052 mL | 2.5261 mL | 5.0523 mL | |
| 10 mM | 0.2526 mL | 1.2631 mL | 2.5261 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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