Cat. No.: HY-10581

Gatifloxacin

(Synonyms: AM-1155; BMS-206584; PD135432)

4 Cited Publications

Customer Review

Based on 4 publication(s) in Google Scholar

Gatifloxacin (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic that can cross the blood-brain barrier, with broad-spectrum antibacterial activity. Gatifloxacin inhibits bacterial type II topoisomerases (IC₅₀=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC₅₀=0.109 μg/ml). Gatifloxacin can be used to treat bacterial conjunctivitis in vivo.

For research use only. We do not sell to patients.

Purity: 99.69%
CAS No.: 112811-59-3
Formula: C₁₉H₂₂FN₃O₄
Molecular Weight:375.39

Storage:

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Gatifloxacin Chemical Structure

CAS No.: 112811-59-3

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (4)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Gatifloxacin (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic that can cross the blood-brain barrier, with broad-spectrum antibacterial activity. Gatifloxacin inhibits bacterial type II topoisomerases (IC₅₀=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC₅₀=0.109 μg/ml)^[1]. Gatifloxacin can be used to treat bacterial conjunctivitis in vivo.

IC₅₀ & Target^[1]

Quinolone

Topoisomerase II

36.7 μM (IC₅₀)

All Topoisomerase Isoforms :

All Antibiotic Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	400 μM Compound: Gatifloxacin	Inhibition of human HeLa cell proliferation Inhibition of human HeLa cell proliferation	[PMID: 19595598]
HEp-2	CC₅₀	67 μM Compound: gatifloxacin	Cytotoxicity against human Hep2 laryngeal carcinoma cell line Cytotoxicity against human Hep2 laryngeal carcinoma cell line	[PMID: 16337791]
MDCK	CC₅₀	396 μM Compound: GTFX	Cytotoxicity against MDCK cells after 48 hrs by CPE assay Cytotoxicity against MDCK cells after 48 hrs by CPE assay	[PMID: 21481984]
MRC5	IC₅₀	12.7 μM Compound: GTFX (gatifloxacin)	In vitro inhibitory activity on MRC5 fibroblast tissue cultures inoculated with virulent RH strain of Toxoplasma gondii In vitro inhibitory activity on MRC5 fibroblast tissue cultures inoculated with virulent RH strain of Toxoplasma gondii	[PMID: 15125930]
NIH3T3	IC₅₀	596 μM Compound: 5	Cytotoxicity against mouse NIH/3T3 cells after 72 hrs by MTT assay Cytotoxicity against mouse NIH/3T3 cells after 72 hrs by MTT assay	[PMID: 18950903]
T-cell	IC₅₀	>50 μg/mL Compound: GTX	Anti-inflammatory activity in Homo sapiens (human) T lymphocytes assessed as inhibition of PHA-induced [3H] thymidine uptake incubated for 72 hr prior to [3H]thymidine addition measured after 18 hr by liquid scintillation method Anti-inflammatory activity in Homo sapiens (human) T lymphocytes assessed as inhibition of PHA-induced [3H] thymidine uptake incubated for 72 hr prior to [3H]thymidine addition measured after 18 hr by liquid scintillation method	10.1007/s00044-009-9264-y
V79	IC₅₀	85 μg/mL Compound: 10c	Clonogenic cytotoxicity against Chinese hamster V-79 cells Clonogenic cytotoxicity against Chinese hamster V-79 cells	[PMID: 7473575]
Vero	CC₅₀	>155.3 μM Compound: Gati	Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay	[PMID: 18502542]
Vero	CC₅₀	125 μg/mL Compound: GTFX	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 28646656]
Vero	CC₅₀	125 μg/mL Compound: GTFX	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 28720502]
Vero	CC₅₀	64 μg/mL Compound: Gatifloxacin	Cytotoxicity against African green monkey Vero cells incubated for 72 hrs by MTT assay Cytotoxicity against African green monkey Vero cells incubated for 72 hrs by MTT assay	[PMID: 31352245]
Vero	IC₅₀	>155.3 μM Compound: Gati	Cytotoxicity against Vero cells after 72 hrs by MTT assay Cytotoxicity against Vero cells after 72 hrs by MTT assay	[PMID: 17960928]
Vero	IC₅₀	>155.3 μM Compound: Gati	Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay	[PMID: 18304818]
Vero	IC₅₀	>155.3 μM Compound: gatifloxacin	Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay	[PMID: 18078756]
Vero	IC₅₀	>159.5 μM Compound: Gatifloxacin	Cytotoxicity against Chlorocebus aethiops (African green monkey) Vero cells after 72 hr Cytotoxicity against Chlorocebus aethiops (African green monkey) Vero cells after 72 hr	10.1007/s00044-010-9322-5
Vero	IC₅₀	>550 μM Compound: Gatifloxacin	Cytotoxicity against Chlorocebus aethiops (African green monkey) Vero cells after 72 hr by MTT assay Cytotoxicity against Chlorocebus aethiops (African green monkey) Vero cells after 72 hr by MTT assay	10.1007/s00044-011-9646-9
Vero	IC₅₀	>62.5 μg/mL Compound: Gati	Cytotoxicity against Vero cell line Cytotoxicity against Vero cell line	[PMID: 16759086]

In Vitro

Gatifloxacin is against S. aureus MS5935 topoisomerase IV, E. coli NIHJ JC-2 DNA gyrase and HeLa cell topoisomerase II with IC₅₀ values of 13.8 μg/ml, 0.109 μg/ml, and 265 μg/ml, respectively^[1].
Gatifloxacin is against S. aureus MS5935 topoisomerase IV, E. coli NIHJ JC-2 DNA gyrase and HeLa cell topoisomerase II with MIC values of 0.05 μg/ml, 0.0063 μg/ml, and 122 μg/ml, respectively^[1].
Gatifloxacin exhibits antibacterial activities for wild-type strains (MS5935, MS5952, MR5867 and MR6009) the first-, second-, third-, and fourth-step mutants with MIC values of 0.05 to 0.10 μg/ml, 0.20 μg/ml, 1.56 to 3.13 μg/ml, 1.56 to 6.25 μg/ml, and 50 to 200 μg/ml, respectively. Gatifloxacin displays the most potent activity against the second- and third-step mutants (MS5952, MR5867 and MR6009) except for the second-step mutant of strain MS5935^[2].
Gatifloxacin has potent activity against norA transformant NY12 (MIC, 0.39 μg/ml)^[2].
Gatifloxacin (20-100 μM; 72 hours) significantly decreases insulin content to 60% at Day 1, and continues to be reduced to 50.1% and 44.7% at Day 3 by 20 μM and 100 μM gatifloxacin, respectively^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Gatifloxacin (subcutaneous injection; 100 mg/kg; 3 times a day; 30 days) significantly decreases the number of lesions in mouse footpad with Nocardia brasiliensis^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female BALB/c mice with Nocardia brasiliensis in the right hind footpad.
Dosage:

100 mg/kg
Administration:

Subcutaneous injection; 3 times a day; 30 days
Result:

Reduced the production of lesions in mice.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 112811-59-3
Appearance Solid
Molecular Weight 375.39
Formula C₁₉H₂₂FN₃O₄
Color White to off-white
SMILES

CC1NCCN(C2=C(F)C=C3C(N(C4CC4)C=C(C(O)=O)C3=O)=C2OC)C1
Synonyms

AM-1155; BMS-206584; PD135432
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Publications (4)

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Journal Impact Factor

J Appl Toxicol

Reactive metabolite of trovafloxacin activates inflammasomes: Implications for trovafloxacin-induced liver injury. [Abstract]

2024 Jun;44(6):846-852. PMID: 38291012
Ghent university
bioRxiv

2020 Jun.
Patent

US20180263995A1.

Solvent & Solubility

In Vitro:

DMSO : 2 mg/mL (5.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 1 mg/mL (2.66 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6639 mL

13.3195 mL

26.6390 mL

5 mM

0.5328 mL

2.6639 mL

5.3278 mL

10 mM

---

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Takei M, et al. Inhibitory activities of gatifloxacin (AM-1155), a newly developed fluoroquinolone, against bacterial and mammalian type II topoisomerases.Antimicrob Agents Chemother. 1998 Oct;42(10):2678-81. [Content Brief]

[2]. Fukuda H, et al. Antibacterial activity of gatifloxacin (AM-1155, CG5501, BMS-206584), a newly developed fluoroquinolone, against sequentially acquired quinolone-resistant mutants and the norA transformant of Staphylococcus aureus. Antimicrob Agents Chemother. 1998 Aug;42(8):1917-22. [Content Brief]

[3]. Yamada C, et al. Gatifloxacin acutely stimulates insulin secretion and chronically suppresses insulin biosynthesis. Eur J Pharmacol. 2006 Dec 28;553(1-3):67-72. Epub 2006 Sep 28. [Content Brief]

[4]. Lutsar I, et al. Pharmacodynamics of gatifloxacin in cerebrospinal fluid in experimental cephalosporin-resistant pneumococcal meningitis. Antimicrob Agents Chemother. 1998 Oct;42(10):2650-5. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	2.6639 mL	13.3195 mL	26.6390 mL	66.5974 mL
DMSO	5 mM	0.5328 mL	2.6639 mL	5.3278 mL	13.3195 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Gatifloxacin

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Publications Citing Use of MedChemExpress (MCE) Gatifloxacin

All Topoisomerase Isoforms

All Antibiotic Isoforms