Carbimazole 是咪唑类甲状腺拮抗试剂,在体内快速转化为 MMI 而发挥作用,在体外可转化为甲咪唑,可用于 Graves 病的研究。
产品描述
Carbimazole is an imidazole antithyroid agent. It is only found in individuals that have used or taken this drug. Carbimazole is metabolized to methimazole, which is responsible for the antithyroid activity. Carbimazole is an antithyroid agent that decreases the uptake and concentration of inorganic iodine by the thyroid, it also reduces the formation of di-iodotyrosine and thyroxine. Once converted to its active form of methimazole, it prevents the thyroid peroxidase enzyme from coupling and iodinating the tyrosine residues on thyroglobulin, hence reducing the production of the thyroid hormones T3 and T4.
体内活性
Carbimazole被人体吸收后转化为甲巯咪唑,产生抗甲状腺作用,作用于抗甲亢(过度产生甲状腺激素)和甲状腺毒症(甲状腺炎症)。
激酶实验
In vitro kinase assays: with purified proteins, recombinant S6 protein and recombinant active P70S6K are incubated in 1x kinase buffer with various amount of HCQ or RAD001 in the presence (25 μM) or absence of ATP for 30 minutes at 30°C. Total and phosphorylated S6 at ser235/236 and ser240/244 are detected by western analysis using phosphospecific antibodies. Note that recombinant GST-tagged S6 (53 kd) is distinguished from endogenous S6 (32 kd) on the western blot.
Cas No.
22232-54-8
分子式
C7H10N2O2S
分子量
186.23
别名
卡比马唑;Carbimazol;Athyromazole;卡比吗唑;Neomercazole
储存和溶解度
Ethanol:12 mg/mL (64.4 mM)
DMSO:36 mg/mL (193.3 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years