Telacebec是一种针对结核分枝杆菌(Mycobacterium tuberculosis)细胞色素bc1的抑制剂,这是一种细菌酶复合体,对细菌的呼吸作用至关重要。
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描述 | Imidazopyridine amide as inhibitor of Mycobacterium tuberculosis by targeting its respiratory cytochrome bc1 complex. Telacebec effectively suppresses the growth of both MDR and XDR Mycobacterium tuberculosis strains in culture broth, exhibiting potency in the low nanomolar range. Against the benchmark strain Mycobacterium tuberculosis H37Rv, Telacebec shows MIC50s of 2.7 nM in culture broth and 0.28 nM within macrophages[1]. |
Animal study | Telacebec has been shown to be effective in a mouse tuberculosis model at doses under 1 mg/kg. It is suitable for once-daily administration due to its pharmacokinetic and safety profiles. The bioavailability of Telacebec is high at 90%, and it has a terminal half-life of 23.4 hours. Following a 4-week treatment regimen, Telacebec at dosages of 0.4, 2, and 10 mg/kg resulted in bacterial load reductions of 90%, 99%, and 99.9% respectively, in M. tuberculosis H37Rv[1]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
1.80mL 0.36mL 0.18mL |
8.98mL 1.80mL 0.90mL |
17.95mL 3.59mL 1.80mL |
CAS号 | 1334719-95-7 |
分子式 | C29H28ClF3N4O2 |
分子量 | 557.01 |
SMILES Code | O=C(C1=C(CC)N=C2C=CC(Cl)=CN21)NCC3=CC=C(N4CCC(C5=CC=C(OC(F)(F)F)C=C5)CC4)C=C3 |
MDL No. | MFCD28502122 |
别名 | Q203; IAP6 |
运输 | 蓝冰 |
InChI Key | OJICYBSWSZGRFB-UHFFFAOYSA-N |
Pubchem ID | 68234908 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry, 2-8°C |
溶解方案 |
DMSO: 18 mg/mL(32.32 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |