(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.
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- CAS No.: 2999672-72-7
- Formule: C28H35F3N4O3
- Masse moléculaire:532.60
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
IC50 & Target
EC50: 1.5 μM (SaClpP), 31.4 μM (HsClpP)[1]
Kd: 2.5 μM (SaClpP)[1]
In Vitro
(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. .
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Cell Line:Cell lysates of S. aureus 8325-4 clpP knockout (ΔclpP) strain
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Concentration:0, 2.5, 5 and 10 μM
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Incubation Time:15 min
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Result:SaFtsZ protein was degraded when SaClpP was added.
In Vivo
(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.
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Animal Model:Zebrafish USA300 infection model[1]
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Dosage:25, 50, or 100 mg/kg
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Administration:Intraperitoneal injection, single dose
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Result:Significantly prolong the survival rate at 50 mg/kg. Lost therapeutic effects on zebrafish infected with the ΔclpP mutant strain.
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Animal Model:Female BALB/c mice, S. aureus infection model[1]
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Dosage:7.5 mg/kg
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Administration:Subcutaneous injection, twice a day for 3 days
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Result:Caused a smaller necrotic lesion size in mice compared with the vehicle control.
Chemical Information
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CAS No. 2999672-72-7
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Masse moléculaire 532.60
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Formule C28H35F3N4O3
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
(R)-ZG197 Related Classifications
HY-152096 Related Classifications
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