Ethionamide,536-33-4

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产品名称：Ethionamide

产品别名：乙硫异烟胺

英文别名：2-ethylthioisonicotinamide

靶点：Antibacterial

CAS：536-33-4

纯度：>98%

外观：微黄色结晶性粉末

保存方法：-20°C

描述：

Ethionamide (2-ethylthioisonicotinamide) is an antibiotic used in the treatment of tuberculosis. It works by inhibiting or stopping the growth of TB cells, which results in cell death.

溶解性：Ethanol ：14 mg/mL (84.2 mM)
DMSO ：31 mg/mL (186.5 mM)

体外研究：

Ethionamide is a structural analogue of isoniazid (INH), both are pro-drugs that need to be activated by mycobacterial enzymes to exert their antimicrobial activity. Ethionamide mechanism of action is thought to be identical to INH although the pathway of activation is distinct from that of INH. Ethionamide is activated by an EthA enzyme, leading to the formation of a Soxide metabolite that has considerably better activity than the parent drug. Ethionamide inhibits both biofilm formation and viability of mature biofilms. Ethionamide reduces the content of ergosterol in Cryptococcus spp. planktonic cells and destabilized or permeabilized the fungal cell membrane, leading to leakage of macromolecules. Ethionamide is in general toxic at concentrations above 0.50 mM to HepG2, Caco-2, and RAW macrophage cells, but the toxicity is drastically reduced when Ethionamide is loaded into the microparticles. Ethionamide shows a fast metabolization process in the presence of the thermally carbonized- Porous silicon (TCPSi) particles. Ethionamide is activated in Mycobacterium tuberculosis by the protein encoded by the gene Rv3854c. Ethionamide appear to disrupt cell wall biosynthesis and have at least one common cellular target, the enoyl-acyl carrier protein reductase InhA.

体内研究：

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