(R)-ZG197
(R)-ZG197 is a highly selective Staphylococcus aureus Caseinolytic protease P (SaClpP) activator with an EC50 of 1.5 μM. (R)-ZG197 also activates Homo sapiens ClpP (HsClpP) with an EC50 of 31.4 μM.
For research use only. We do not sell to patients.
- CAS No.: 2999672-72-7
- Formula: C28H35F3N4O3
- Molecular Weight:532.60
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
EC50: 1.5 μM (SaClpP), 31.4 μM (HsClpP)[1]
Kd: 2.5 μM (SaClpP)[1]
(R)-ZG197 (10 μM; 2 h) significantly enhances the thermal stability of SaClpP while having a weak effect on HsClpP[1].
(R)-ZG197 (0-256 μg/mL; 18 h) significantly suppresses S. aureus with a quantified MIC of 0.5 μg/mL. (R)-ZG197 displays strong antibacterial activity on a broad spectrum of S. aureus strains, with MIC values of 0.5-2 μg/mL[1].
(R)-ZG197 (0-20 μM) decrease SaFtsZ abundance in the 8325-4 S. aureus but not in the corresponding ΔclpP mutant strain[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Cell lysates of S. aureus 8325-4 clpP knockout (ΔclpP) strain
-
Concentration:0, 2.5, 5 and 10 μM
-
Incubation Time:15 min
-
Result:SaFtsZ protein was degraded when SaClpP was added.
(R)-ZG197 (7.5 mg/kg; s.c.; twice a day for 3 days) shows anti-infective efficacy in murine skin S. aureus infection models[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Zebrafish USA300 infection model[1]
-
Dosage:25, 50, or 100 mg/kg
-
Administration:Intraperitoneal injection, single dose
-
Result:Significantly prolong the survival rate at 50 mg/kg. Lost therapeutic effects on zebrafish infected with the ΔclpP mutant strain.
-
Animal Model:Female BALB/c mice, S. aureus infection model[1]
-
Dosage:7.5 mg/kg
-
Administration:Subcutaneous injection, twice a day for 3 days
-
Result:Caused a smaller necrotic lesion size in mice compared with the vehicle control.
Chemical Information
-
CAS No. 2999672-72-7
-
Molecular Weight 532.60
-
Formula C28H35F3N4O3
-
SMILES
O=C(N1CCC(N([C@H]2[C@@H](C)CC)[C@]1([H])CN([C@H](C)C3=C(C=CC=C4)C4=CC=C3)C2=O)=O)NCCCC(F)(F)F
-
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)
Powered by Bioz