1. Anti-infection
  2. Bacterial
  3. Antituberculosis agent-9

Antituberculosis agent-9 (Compound 5a) is an orally active antitubercular agent with an MIC of 0.5 μg/mL against H37Ra.

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Antituberculosis agent-9

Antituberculosis agent-9 Chemical Structure

CAS No. : 2998587-72-5

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Description

Antituberculosis agent-9 (Compound 5a) is an orally active antitubercular agent with an MIC of 0.5 μg/mL against H37Ra[1].

Cellular Effect
Cell Line Type Value Description References
HepG2 IC50
3.1 μM
Compound: 5a
Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 36735271]
In Vitro

Antituberculosis agent-9 (Compound 5a; 48 h) shows cytotoxicity against HepG2 cells with an IC50 value of 3.1 μM[1].
Antituberculosis agent-9 (6 days) also shows inhibitory activities against MRSA, M. abscessus and M. smegmatis with MICs of 4.0 μg/mL[1].
Antituberculosis agent-9 (6 days) shows inhibitory activities against clinical isolates of M. tuberculosis with MICs of 0.5, 0.5, 0.5, 1.0 and 1.0 μg/mL for H37Rv, K4, K12, K5 and K16, respectively[1].

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

In Vivo

Antituberculosis agent-9 (Compound 5a; 300 mg/kg; oral; daily for 4 days) shows moderate antitubercular efficacy in mice[1].

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

Animal Model: Female BALB/c mice, autoluminescent Mtb infection model[1]
Dosage: 300 mg/kg
Administration: Oral administration, daily for 4 days
Result: There was a relative light unit (RLU) reduction of 0.5 log10 in live mice, compared to the control group (CMC-Na).
Animal Model: Sprague-Dawley rats[1]
Dosage: 5 or 15 mg/kg
Administration: IV or PO (Pharmacokinetic Analysis)
Result: Pharmacokinetic Parameters of Antituberculosis agent-9 (Compound 5a) In Vivo[1]
cpd. administration Cmax (μg/L) Tmax (h) T1/2 (h) Clz (L/h/kg) AUC0-t (μg/L•h) F %
Antituberculosis agent-9 (Compound 5a) iv (5 mg/kg) 595 ± 62 26.2 ± 0.9 1.5 ± 0.3 1694 ± 201
po (15 mg/kg) 108 ± 18 >24 2079 ± 274 40.7
Molecular Weight

436.98

Formula

C25H29ClN4O

CAS No.
SMILES

CC1=C(C2CCNCC2)C=C(OC(C)C)C(NC3=C(Cl)C=NC(C4=CC=CC=C4)=N3)=C1

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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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Antituberculosis agent-9 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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Product Name:
Antituberculosis agent-9
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HY-149064
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