Thiacetazone (Thioacetazone) is a thiourea-containing antitubercular agent and is an orally active antibiotic. Thiacetazone has antibacterial action, which inhibits growth of Mycobacterium tuberculosis H37Rv with a MIC value of 0.1 μg/mL.
性状
Solid
IC50 & Target[1][2]
MIC: 0.1 μg/mL (Mycobacterium tuberculosis H37Rv)
体外研究(In Vitro)
Thiacetazone is a prodrug that is activated by the mycobacterial monooxygenase EthA, which is also the activator of two other anti-tuberculosis agents, Ethionamide and Isoxyl. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
The K m and V max values for the N-deacetylation of Thiacetazone are 0.57 mM and 0.123 nmol of p-aminobenzaldehydethiosemicarbazone formed/min/mg cytosolic protein, respectively. The ability to metabolize Thiacetazone is the same in the livers of cat, mouse and human, but lagged significantly in that of rat. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. J L Stigliani, et al. New Insights Into the Chemical Behavior of S-oxide Derivatives of Thiocarbonyl-Containing Antitubercular Drugs and the Influence on Their Mechanisms of Action and Toxicity. Ann Pharm Fr. 2019 Mar;77(2):126-135.[2]. P Khanna, et al. Characteristics of a Cytosolic Arylacylamidase Metabolizing Thiacetazone. J Pharmacol Exp Ther. 1992 Sep;262(3):1225-31.
溶解度数据
In Vitro: DMSO : 100 mg/mL (423.21 mM; Need ultrasonic)配制储备液