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编 号：F762511
分子式：C25H29ClN4O
分子量：436.98
分子式：C25H29ClN4O
分子量：436.98
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CAS No: 2998587-72-5
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生物活性：
Antituberculosis agent-9 (Compound 5a) is an orally active antitubercular agent with an MIC of 0.5 μg/mL against H37Ra.
体内研究：
Antituberculosis agent-9 (Compound 5a; 300 mg/kg; oral; daily for 4 days) 对小鼠有中等抗结核作用。Animal Model:Female BALB/c mice, autoluminescent Mtb infection model
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
Dosage:5 or 15 mg/kg
Administration:IV or PO (Pharmacokinetic Analysis)
Result:Pharmacokinetic Parameters of Antituberculosis agent-9 (Compound 5a) In Vivocpd.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 ± 6226.2 ± 0.91.5 ± 0.31694 ± 201
po (15 mg/kg)108 ± 18>242079 ± 27440.7
体外研究：
Antituberculosis agent-9 (Compound 5a; 48 h) 显示出对 HepG2 细胞的细胞毒性，IC50 值为 3.1 μM。Antituberculosis agent-9 (6 days) 对 MRSA、M. abscessus 和 M. smegmatis 有抑制作用，MIC 均为 4.0 μg/mL。Antituberculosis agent-9 (6 days) 对临床分离的 M. tuberculosis 有抑制作用。对 H37Rv、K4、K12、K5、K16 的 MIC 值分别为 0.5、0.5、0.5、1.0 和 1.0 μg/mL。
Antituberculosis agent-9 (Compound 5a) is an orally active antitubercular agent with an MIC of 0.5 μg/mL against H37Ra.
体内研究：
Antituberculosis agent-9 (Compound 5a; 300 mg/kg; oral; daily for 4 days) 对小鼠有中等抗结核作用。Animal Model:Female BALB/c mice, autoluminescent Mtb infection model
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
Dosage:5 or 15 mg/kg
Administration:IV or PO (Pharmacokinetic Analysis)
Result:Pharmacokinetic Parameters of Antituberculosis agent-9 (Compound 5a) In Vivocpd.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 ± 6226.2 ± 0.91.5 ± 0.31694 ± 201
po (15 mg/kg)108 ± 18>242079 ± 27440.7
体外研究：
Antituberculosis agent-9 (Compound 5a; 48 h) 显示出对 HepG2 细胞的细胞毒性，IC50 值为 3.1 μM。Antituberculosis agent-9 (6 days) 对 MRSA、M. abscessus 和 M. smegmatis 有抑制作用，MIC 均为 4.0 μg/mL。Antituberculosis agent-9 (6 days) 对临床分离的 M. tuberculosis 有抑制作用。对 H37Rv、K4、K12、K5、K16 的 MIC 值分别为 0.5、0.5、0.5、1.0 和 1.0 μg/mL。
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