MCR-1-IN-1
MCR-1-IN-1 is an MCR-1 inhibitor with a Kd of 54 μM for E. coli MCR-1. MCR-1-IN-1 alone shows no significant growth inhibition against Mcr-1-positive E. coli. MCR-1-IN-1 produces a synergistic effect with Colistin in Mcr-1-positive E. coli, restoring Colistin sensitivity. MCR-1-IN-1 combined with Colistin improves survival and reduces bacterial burden in a mouse peritonitis infection model.
For research use only. We do not sell to patients.
- CAS No.: 3046153-44-7
- Formula: C27H33BrClN3O3
- Molecular Weight:562.93
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HK-2 | IC50 |
4.6 μM
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Cytotoxicity against human HK-2 cells assessed as viability reduction incubated 24 hrs by CCK-8 assay at 450 nm.
Cytotoxicity against human HK-2 cells assessed as viability reduction incubated 24 hrs by CCK-8 assay at 450 nm.
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42917914 |
| LX-2 | IC50 |
4.8 μM
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Cytotoxicity against human LX-2 cells assessed as viability reduction incubated 24 hrs by CCK-8 assay at 450 nm.
Cytotoxicity against human LX-2 cells assessed as viability reduction incubated 24 hrs by CCK-8 assay at 450 nm.
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42917914 |
In Vitro
MCR-1-IN-1 (7 µM; 6-24 h) accumulates up to 152-fold in HeLa cells[1].
MCR-1-IN-1 (0-50 µM; 16 h) restores Colistin susceptibility in mcr-1-positive E. coli in a dose-dependent manner, and at 50 µM combined with 4 µg/mL Colistin, all 12 strains are killed[1].
MCR-1-IN-1 (12.5-100 µM; 16 h) alone shows no inhibitory effect on mcr-1-positive E. coli at 12.5-100 µM, and its MIC against ATCC 25922 is 50 µM[1].
MCR-1-IN-1 (7 µM; 3-7 h) synergizes with Colistin to reduce the CFU of E. coli 18QY096[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549, HeLa, HK-2, and LX-2 cells
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Concentration:0, 2, 4, 8, 16, 32, and 64 µM
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Incubation Time:24 h
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Result:In A549 cells, no significant cytotoxicity was observed at ≤32 µM, and more than half of the cells died at 64 µM.
In HeLa cells, no significant cytotoxicity was observed at ≤16 µM, and viability significantly decreased at 32 µM.
IC50 values were 4.6 µM in HK-2 cells and 4.8 µM in LX-2 cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 5-7 weeks old, 20 g)[1]
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Dosage:2 mg/kg (alone); 2 mg/kg plus 0.5 mg/kg colistin (combination)
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Administration:i.p.; single dose immediately after infection
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Result:At 72 h postinfection, single-agent groups had 12.5% survival.
Co-administration with colistin (0.5 mg/kg) increased survival to 37.5%.
At 24 h postinfection, the combination group had lower bacterial loads in liver, spleen, and kidneys than the other groups.
Chemical Information
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CAS No. 3046153-44-7
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Molecular Weight 562.93
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Formula C27H33BrClN3O3
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SMILES
N#CC1=C(N)OC2=C(C=CC(OCC(O)CNCCCCCCCC)=C2)C1C3=CC=C(Cl)C(Br)=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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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)
MCR-1-IN-1 Related Classifications
HY-190737 Related Classifications
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