TCA-1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

具有抗耐药性和持续性结核病活性的小分子；在体外显示出针对非复制 Mtb 的杀菌活性，并且在急性和慢性 Mtb 感染小鼠模型中有效。

A small molecule with activity against drug-resistant and persistent tuberculosis; shows bactericidal activity against nonreplicating Mtb in vitro and is efficacious in acute and chronic Mtb infection mouse models; down-regulates genes known to be involved in Mtb persistence; inhibits DprE1 and MoeW, enzymes involved in cell wall and molybdenum cofactor biosynthesis.

TCA1 shows bactericidal activity against both replicating (WT and drug resistant) and nonreplicating Mycobacterium tuberculosis (Mtb). TCA1 inhibits biofilm formation by Mtb H37Rv. TCA1 shows selective inhibitory activity against bacterial growth-it is inactive against Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa, suggesting that the target for its bactericidal activity is specific to the genus Mycobacterium.

TCA1 (40 mg/kg; oral gavage; 1 time/d for 5 d/week; for 4 weeks) is efficacious in acute and chronic Mtb infection mouse models.In a mouse model of Mtb infection, after i.v. administration, TCA1 exhibits a low clearance and steady-state volume of distribution, with an elimination half-life of 0.73 h. After oral administration of 20 and 50 mg/kg in solution formulation, TCA1 shows a high Cmax (2122 and 5653 nM, respectively), moderate exposure with oral bioavailability ranging from 19% to 46%, and a half-life of 1.8 h.

TCA1

GPCR/G Protein

Antibacterial

Antibacterial

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864941-32-2

375.417

C16H13N3O4S2

>98% (HPLC)

DMSO: Soluble （ < 1 mg/ml refers to the product slightly soluble or insoluble )

CCOC(=O)NC(=O)C1=C(SC=C1)NC(=O)C2=NC3=CC=CC=C3S2

ethyl (2-(benzo[d]thiazole-2-carboxamido)thiophene-3-carbonyl)carbamate

(-20℃)

With Ice Pack

≥ 2 years