DNA Gyrase/ribosomes-IN-1
DNA Gyrase/ribosomes-IN-1 is a bacterial ribosome and DNA gyrase inhibitor, with IC50 values of 1.11 μM and 3.31 μM, respectively. DNA Gyrase/ribosomes-IN-1 also inhibits CYP3A4, with an IC50 of 18.5 μM, and exhibits stability in mouse plasma and liver microsomes. DNA Gyrase/ribosomes-IN-1 inhibits bacterial protein synthesis by interacting with ribosomal RNA and associated sites. DNA Gyrase/ribosomes-IN-1 suppresses bacterial DNA replication by interacting with the gyrase complex. DNA Gyrase/ribosomes-IN-1 restores activity against macrolide-resistant, erm-mediated Gram-positive pathogens and enhances activity against Gram-negative bacteria such as Haemophilus influenzae and Moraxella catarrhalis. DNA Gyrase/ribosomes-IN-1 can be used in research on community-acquired bacterial pneumonia.
For research use only. We do not sell to patients.
- Formula: C53H77F2N5O14
- Molecular Weight:1046.20
-
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
All DNA/RNA Synthesis Isoforms
More
Biological Activity
Description
IC50 & Target
|
CYP3A4 18.5 μM (IC50) |
In Vitro
DNA Gyrase/ribosomes-IN-1 (compound 26l) (0.01-5 μM) inhibits E. coli protein synthesis with an IC50 of 1.11 μM and E. coli DNA gyrase with an IC50 of 3.31 μM, demonstrating dual inhibition of these two targets[1].
DNA Gyrase/ribosomes-IN-1 (0.01-30 μM) inhibits CYP3A4 with an IC50 of 18.5 μM[1].
DNA Gyrase/ribosomes-IN-1 (1 μM) exhibits high stability in mouse plasma (99.30% remaining after 0.5 h) and moderate stability in mouse liver microsomes (75.82% remaining after 1 h)[1].
DNA Gyrase/ribosomes-IN-1 (10-50 μM; 48 h) exhibits cytotoxicity with CC50 values of 25.77 μM in HepG2 cells and 23.40 μM in 293T cells[1].
DNA Gyrase/ribosomes-IN-1 (0.008-256 μg/mL; 16-24 h) exhibits antibacterial activity against various strains including S. pneumoniae, S. pyogenes, and H. influenzae with MIC values ranging from 0.03 to 0.5 μg/mL[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:HepG2, 293T
-
Concentration:10 μM, 50 μM
-
Incubation Time:48 h
-
Result:Exhibited a CC₅₀ of 25.77 μM in HepG2 cells. Exhibited a CC₅₀ of 23.40 μM in 293T cells.
Parmacokinetics
| Species | Dose | Route | Cmax | Tmax | T1/2 | AUC0-24 | AUC0-∞ | CL | MRT |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 5 mg/kg | i.v. | 221.2 ng/mL | 0.08 h | 7.7 h | 562.0 ng·h/mL | 617.4 ng·h/mL | 8105.9 mL/h/kg | 5.5 h |
Chemical Information
-
Molecular Weight 1046.20
-
Formula C53H77F2N5O14
-
SMILES
C[C@H]1C([C@](C)(F)C(O[C@H](CC)[C@@](C)(O2)[C@H](N(CCCN3[C@@H](C)CN(C4=C(OC)C(N(C5CC5)C=C(C(O)=O)C6=O)=C6C=C4F)CC3)C2=O)[C@@H](C)C([C@H](C)C[C@@](C)(OC)[C@@H]1O[C@H]7[C@H](O)[C@@H](N(C)C)C[C@H](C)O7)=O)=O)=O
-
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)
DNA Gyrase/ribosomes-IN-1 Related Classifications
HY-181107 Related Classifications
Powered by Bioz