Mtb ATP synthase-IN-1

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CAS NO:

2642394-38-3

Mtb ATP synthase-IN-1 (compound 6ab) 是一种有效的结核分枝杆菌 (Mtb) ATP 合成抑制剂，对Mtb的 MIC 为 0.452 ~ 0.499 μg/mL。Mtb ATP synthase-IN-1 代谢稳定性好，细胞毒性低 (Vero IC₅₀>64 μg/mL)，具有一定的口服生物利用度。Mtb ATP synthase-IN-1 可用于抗结核分枝杆菌的研究。

生物活性

Mtb ATP synthase-IN-1 (compound 6ab) is a potentMycobacterium tuberculosis(Mtb)ATP synthaseinhibitor, with MIC of 0.452-0.499 μg/mL againstMtb. Mtb ATP synthase-IN-1 has good metabolic stability, low cytotoxicity (Vero IC₅₀>64 μg/mL), and acceptable oral bioavailability. Mtb ATP synthase-IN-1 can be used for researching anti-mycobacterium^[1].

IC₅₀& Target

MIC: 0.452-0.499 μg/mL (Mtb)^[1]

体内研究
(In Vivo)

Mtb ATP synthase-IN-1 (50 mg/kg for PO, 5 mg/kg for IV; single dosage) exhibits good metabolic stability and acceptable oral bioavailability^[1].
Pharmacokinetic Parameters of Mtb ATP synthase-IN-1 in male CD-1 mouse^[1].

	PO (50 mg/kg)	IV (5 mg/kg)
C_max(ng/mL)	1333	1241
T_max(h)	0.83
T_1/2(h)	0.51	0.33
AUC_0-t(ng/mL·h)	2197	1667
AUC_0-∞(ng/mL·h)	2198	1672
MRT_0-∞(ng/mL)	1.36	0.28
CL (mL/min/kg)		51.4
F (%)	13.1

Animal Model:	Male CD-1 mouse^[1]
Dosage:	50 and 5 mg/kg
Administration:	50 mg/kg for PO, 5 mg/kg for IV; single dosage (Pharmacokinetics Analysis)
Result:	Exhibited good metabolic stability and acceptable oral bioavailability.

分子量

323.30

Formula

C₁₇H₁₃N₃O₄

CAS 号

2642394-38-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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