AM-8722
AM-8722 is an orally active inhibitor of bacterial DNA gyrase and topoisomerase IV. AM-8722 inhibits bacterial DNA synthesis and exhibits broad-spectrum antibacterial activity against Gram-positive and Gram-negative pathogens. AM-8722 can be used for research on bacterial septicemia and bacterial infections.
For research use only. We do not sell to patients.
- CAS No.: 2230715-40-7
- Formula: C27H30ClN5O5
- Molecular Weight:540.01
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
In Vitro
AM-8722 selectively inhibits DNA replication in S. aureus with an IC50 of 1.10 μg/mL[1].
AM-8722 is a potent inhibitor of bacterial DNA gyrase and topoisomerase IV from S. aureus and E. coli, with IC50s of 0.83 μM and 0.14 μM for DNA gyrase, respectively, and is selective against human topoisomerase II[1].
AM-8722 exhibits potent broad-spectrum antibacterial activity against various Gram-positive and Gram-negative organisms, including resistant strains[1].
The antibacterial activity of AM-8722 against S. aureus RN4220 is unaffected by the presence of excess DNA or human serum, with an MIC of 0.125 μg/mL[1].
AM-8722 displays potent in vitro activity against a broad panel of clinical isolates, including Staphylococcus, Acinetobacter, H. influenzae, and M. catarrhalis[1].
AM-8722.HCl exhibits potent and rapid bactericidal activity against S. aureus ATCC 29213 at concentrations of 1 μg/mL and above, with no regrowth at 16× MIC or higher[1].
AM-8722 (compound 6) (0.031-8 μg/mL) shows broad-spectrum antibacterial activity with MIC values of 0.031 μg/mL against Staphylococcus aureus Smith, 0.5 μg/mL against Streptococcus pneumoniae IID553, 2 μg/mL against Enterococcus faecium VanA (VRE), 2 μg/mL against Escherichia coli ATCC 25922, 0.25 μg/mL against Acinetobacter baumannii IID876, and 8 μg/mL against Pseudomonas aeruginosa PAO1[2].
AM-8722 is a substrate for human, rat, and mouse P-glycoprotein (Pgp), as demonstrated by BA/AB ratios of >27.1, >21.5, and 24.7 in LLC-MDR1, LLC-Mdr1a, and LLC-Mdr1a cells, respectively[1].
AM-8722 exhibits high apparent permeability across MDCKII monolayers with a Papp of 23.6 × 10−6 cm/s[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
AM-8722 (3.2-50 mg/kg; p.o.; single administration; 1 h post-inoculation) exhibits an ED50 of 20.6 mg/kg in a mouse MSSA disseminated infection model, and its efficacy level is consistent with the 21%-27% oral bioavailability of the drug in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:CD-1 (female, immunocompetent, intraperitoneal inoculation with methicillin-susceptible Staphylococcus aureus strain Smith)[1]
-
Dosage:3.2-50 mg/kg (i.v.); 3.2-50 mg/kg (p.o.)
-
Administration:i.v.; single dose; 1 h post-inoculation
-
Result:Achieved an ED50 of 2.1 mg/kg intravenously.
Achieved 1-, 2-, and 3-log reductions (ED90, ED99, and ED99.9) in bacterial burden at 6.3, 11.5, and 17.0 mg/kg intravenously, respectively.
Achieved ED50, ED90, ED99, and ED99.9 of 20.6, 31.6, 42.7, and 52.8 mg/kg orally, respectively.
Chemical Information
-
CAS No. 2230715-40-7
-
Molecular Weight 540.01
-
Formula C27H30ClN5O5
-
SMILES
O=C1C=CC2=C(N1CCO)C(CCC34OCC(CC3)(CC4)NCC5=NC(N6)=C(C=C5)OCC6=O)=C(Cl)C=N2
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AM-8722 Related Classifications
HY-187725 Related Classifications
Powered by Bioz