1. Anti-infection
  2. Bacterial
  3. Antituberculosis agent-10

Antituberculosis agent-10 (Compound 9) has excellent antibacterial activity against Mycobacterium tuberculosis (MIC = 0.3 μM). Antituberculosis agent-10 inhibits protein synthesis by targeting the 50S ribosomal subunit of the bacterium, thus exerting its antibacterial effect. Antituberculosis agent-10 is orally active.

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Antituberculosis agent-10 Chemical Structure

Antituberculosis agent-10 Chemical Structure

CAS No. : 2095636-19-2

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Description

Antituberculosis agent-10 (Compound 9) has excellent antibacterial activity against Mycobacterium tuberculosis (MIC = 0.3 μM). Antituberculosis agent-10 inhibits protein synthesis by targeting the 50S ribosomal subunit of the bacterium, thus exerting its antibacterial effect. Antituberculosis agent-10 is orally active[1].

In Vitro

Antituberculosis agent-10 (72 h) is inactive in inhibiting mitochondrial protein synthesis (MPS) in HepG2 cells (IC50 = 150 μM), but its metabolites shows mitochondrial toxicity[1].

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

In Vivo

Antituberculosis agent-10 ((i.g.; 5-50 mg/kg; once or twice a day) exhibits excellent permeability and sustained activity within infected C3HeB/FeJ mice[1].
Antituberculosis agent-10 ((i.g.; 4 mg/kg; twice daily for one week then once daily ) reduces the volume of tuberculosis foci in Mtb-infected marmosets with potent antibacterial activity[1].


Pharmacokinetic Analysis in Antituberculosis agent-10[1]

Route Dose (mpk) Cl/Clu (mL/min/kg) Vd/Vdu (L/kg) MRT/ss t1/2 (h) F (%)
i.v. 2 12/316 0.6/16 0.8/0.6 /
p.o. 10 / / / 64

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

Animal Model: infected C3HeB/FeJ mice[1]
Dosage: 5,10,15,,50 mg/kg, twice daily; 30 mg/kg,once daily
Administration: i.g.
Result: Penetrated effectively into both the cellular and necrotic compartments of the lesions.
Maintained concentrations above the MIC for tuberculosis bacteria at various lesion sites.
Animal Model: Mtb-infected marmosets[1]
Dosage: 4 mg/kg, twice daily for 1 week then 4 mg/kg once daily
Administration: i.g.
Result: Reduced physical lesion size and bacterial load within those lesions.
Showed superior or at least comparable results in reducing lesion volume and bacterial count than linezolid (HY-10394).
Molecular Weight

364.39

Formula

C17H17FN2O4S

CAS No.
Unlabeled CAS

SMILES

O=C1O[C@@H](CN)CN1C2=CC=C(C3=CC=C(S(=O)(C)=O)C=C3)C(F)=C2

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Antituberculosis agent-10 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.

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Antituberculosis agent-10
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HY-163486
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