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 Chemical Structure

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].

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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    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-9
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HY-149064
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