2. Metabolic Enzyme/Protease Anti-infection
  3. Acyltransferase Bacterial
  4. CMX410

CMX410 is an orally active and selective Mycobacterium tuberculosis Pks13 acyltransferase domain inhibitor and anti-bacterial agent. CMX410 reacts with the catalytic serine of the Pks13-AT domain to form a stable β-lactam ring, disables the enzyme’s active site, reduces trehalose monomycolate and trehalose dimycolate levels, triggers cell lysis, and reduces intracellular bacterial burden. CMX410 can be used for the research of tuberculosis.

For research use only. We do not sell to patients.

CMX410

CMX410 Chemical Structure

CAS No. : 3027135-80-1

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CMX410 Related Antibodies

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ACAT1 ACAT2 MGAT2 ACAT DGAT1 DGAT2

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Description

CMX410 is an orally active and selective Mycobacterium tuberculosis Pks13 acyltransferase domain inhibitor and anti-bacterial agent. CMX410 reacts with the catalytic serine of the Pks13-AT domain to form a stable β-lactam ring, disables the enzyme’s active site, reduces trehalose monomycolate and trehalose dimycolate levels, triggers cell lysis, and reduces intracellular bacterial burden. CMX410 can be used for the research of tuberculosis[1][2].

Cellular Effect
Cell Line Type Value Description References
HEK-293T CC50
> 40 μM
Compound: 21b
Cytotoxicity against human HEK293T cells assessed as reduction in cell viability measured after 3 days by CellTiterGlo Luminescent assay
Cytotoxicity against human HEK293T cells assessed as reduction in cell viability measured after 3 days by CellTiterGlo Luminescent assay
[PMID: 38142914]
HepG2 CC50
> 40 μM
Compound: 21b
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 3 days by CellTiterGlo Luminescent assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 3 days by CellTiterGlo Luminescent assay
[PMID: 38142914]
In Vitro

CMX410 (Compound 21b) (0.06 µM) potently inhibits Mycobacterium tuberculosis H37Rv with an MIC of 0.06 µM[1].
CMX410 (>40 µM) shows no cytotoxicity against HEK293T or HepG2 cell lines[1].
CMX410 (6 weeks) is equipotent against drug-susceptible and drug-resistant Mtb clinical isolates, with an MIC90 of 0.039 µM against Mtb H37Rv, and has a narrow spectrum of activity limited to mycobacterial species[2].
CMX410 (0.3-20 µM; 3 days) potently reduces intracellular Mtb burden in THP-1 macrophages, with an EC90 of 0.11 µM[2].
CMX410 (0.39 µM, 20 µM; 21 days, 7 days) demonstrates rapid bactericidal activity against replicating Mtb H37Rv and is active against non-replicating persistent Mtb populations[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CMX410 Related Antibodies
Parmacokinetics
Species Dose Route Cmax Tmax T1/2 AUC0-24 F C0 CL Vd
Mice[1] 20 mg/kg p.o. 9290 ng/mL 1.00 h 2.57 h 47615 ng·h/mL 99.4 % / / /
Mice[1] 3 mg/kg i.v. / / 3.93 h 7085 ng·h/mL / 3314 ng/mL 7.05 mL/min/kg 2.38 L/kg
In Vivo

CMX410 (Compound 21b) (2-20 mg/kg; p.o.; daily; 12 days) exhibits dose-dependent efficacy in an acute mouse tuberculosis model, with a 3.1-log10 reduction in lung bacterial burden at the 20 mg/kg daily oral dose[2].
CMX410 (50 mg/kg; p.o.; twice daily; 5 days per week for 4 weeks) reduces bacterial burden in both lungs and spleens of mice with chronic tuberculosis, with an additive effect when combined with rifampicin that yields a 0.8-log10 greater lung CFU reduction than monotherapy[2].
CMX410 (20 mg/kg; p.o.; daily; 5 days per week for 2 months) protects mice from lethal high-dose tuberculosis infection and reduces lung bacterial burden by 1.6-log10 following 2 months of oral daily treatment at 20 mg/kg[2].
CMX410 (100-1000 mg/kg per day; p.o.; twice daily; 14 days) is well tolerated in Wistar Han rats at oral doses up to 1000 mg/kg per day twice daily for 14 days, with no observed adverse effects[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c mice[2]
Dosage: 2 mg/kg; 7 mg/kg; 20 mg/kg
Administration: p.o.; daily; 12 days
Result: Produced a significant 3.1-log10 reduction in lung CFU compared to untreated controls.
Produced a 2.0-log10 reduction in lung CFU compared to untreated controls.
Produced a smaller reduction in lung CFU compared to untreated controls.
Animal Model: BALB/c mice[2]
Dosage: 50 mg/kg
Administration: p.o.; twice daily; 5 days per week for 4 weeks
Result: Produced a 1.37-log10 reduction in lung CFU compared to untreated controls.
Produced a 2.37-log10 reduction in spleen CFU compared to untreated controls.
When combined with rifampicin, produced an extra 0.8-log10 reduction in lung CFU compared to either drug alone.
Animal Model: BALB/c mice[2]
Dosage: 20 mg/kg
Administration: p.o.; daily; 5 days per week for 2 months
Result: Protected mice from lethal outcome.
Reduced lung bacterial burden by 1.6-log10 after 2 months of treatment.
Animal Model: Wistar Han rats (male and female, 6-7 weeks old, initial body weights 219.8-247.1 g (males) and 143.7-171.3 g (females))[2]
Dosage: 100 mg/kg per day; 300 mg/kg per day; 1000 mg/kg per day
Administration: p.o.; twice daily; 14 days
Result: Observed no treatment-related mortality, adverse clinical signs, body weight changes, food consumption changes, ophthalmology abnormalities, or clinical pathology abnormalities at any dose level.
Established no observed adverse effect level at 1000 mg/kg per day.
Molecular Weight

478.42

Formula

C16H13F3N4O6S2
CAS No.
SMILES

FC1=CC(N2N=C(NS(=O)(C)=O)N=C2)=CC(F)=C1COC3=CC=C(OS(F)(=O)=O)C=C3
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
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CMX410 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CMX4103027135-80-1CMX 410CMX-410AcyltransferaseBacterialDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferasetrehalose dimycolatetrehalose monomycolatecell wall biosynthesispretomanidHEK293THepG2rifampicinTHP-1 macrophagesPks13 acyltransferase domainMycobacterium tuberculosisInhibitorinhibitorinhibit

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