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MAC13243 HCl

Catalog No. T15947   CAS 1071638-38-4

MAC13243 HCl, an inhibitor of LolA, a periplasmic chaperone that transports lipoproteins from the inner membrane to the outer membrane, is an antimicrobial agent with specificity and significant inhibitory effects on Gram-negative bacteria.

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MAC13243 HCl Chemical Structure
MAC13243 HCl, CAS 1071638-38-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 122.00
5 mg In stock $ 297.00
10 mg In stock $ 438.00
25 mg In stock $ 716.00
50 mg In stock $ 997.00
100 mg In stock $ 1,330.00
500 mg In stock $ 2,690.00
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Purity: 98.42%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description MAC13243 HCl, an inhibitor of LolA, a periplasmic chaperone that transports lipoproteins from the inner membrane to the outer membrane, is an antimicrobial agent with specificity and significant inhibitory effects on Gram-negative bacteria.
In vitro We investigated the impact of a prototype drug (MAC13243 HCl) interfering with the Gram-negative outer membrane protein LolA on the faecal microbiota. Faecal suspensions from two healthy human donors were exposed to MAC13243 HCl (16, 32, or 64 mg/L) using an in vitro gut model (CoMiniGut). Samples collected 0, 4, and 8 h after exposure were subjected to viable cell counts, 16S rRNA gene quantification and V3-V4 sequencing using the Illumina MiSeq platform. MAC13243 HCl exhibited concentration-dependent killing of coliforms in both donors after 8 h. Concentrations of ≤32 mg/L reduced the growth of aerobic bacteria without influencing the microbiota composition and diversity. An expansion of Firmicutes at the expense of Bacteroidetes and Actinobacteria was observed in the faecal microbiota from one donor following exposure to 64 mg/L of MAC13243 HCl. At all concentrations tested, MAC13243 HCl did not lead to the proliferation of Escherichia coli nor a reduced abundance of beneficial bacteria, which are typical changes observed in antibiotic-induced dysbiosis. These results support our hypothesis that a drug interfering with a specific target in Gram-negative bacteria has a low impact on the commensal gut microbiota and, therefore, a low risk of inducing dysbiosis.[3]
Molecular Weight 442.4
Formula C20H25Cl2N3O2S
CAS No. 1071638-38-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (113.02 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Barker CA, et al. Degradation of MAC13243 and studies of the interaction of resulting thiourea compounds with the lipoprotein targeting chaperone LolA. Bioorg Med Chem Lett. 2013 Apr 15;23(8):2426-31. 2. Pathania R, et al. Chemical genomics in Escherichia coli identifies an inhibitor of bacterial lipoprotein targeting. Nat Chem Biol. 2009 Nov;5(11):849-56. 3. Svanberg Frisinger F, et al. Impact of the Gram-Negative-Selective Inhibitor MAC13243 on In Vitro Simulated Gut Microbiota. Pharmaceuticals (Basel). 2022 Jun 9;15(6):731.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

MAC13243 HCl 1071638-38-4 Microbiology/Virology Antibacterial MAC-13243 MAC13243 inhibitor inhibit

 

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