产品
编 号:F491134
分子式:C24H24N2O5
分子量:420.46
产品类型
结构图
CAS No: 87344-06-7
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产品详情
生物活性:
Amtolmetin guacil is an effective nonsteroidal anti-Inflammatory agent with pain-relieving effects. Amtolmetin guacil inhibits prostaglandin synthesis and cyclooxygenase (COX). Amtolmetin guacil can stimulate capsaicin receptors present on the gastrointestinal wall and also releases gastroprotective nitric oxide (NO). Amtolmetin guacil can be used to research knee osteoarthritis.
体内研究:
Animal Model:Male Wistar rats
Dosage:50 mg/kg
Administration:p.o.; single dosage
Result:Pharmacokinetic Parameters of Amtolmetin guacil in male Wistar rats.AUC0-t (ng/mL·h)AUC0-∞ (ng/mL·h)Cmax (μg/mL)Tmax (h)Kel (h-1)t1/2,β (h)
TMT followingAmtolmetin guacil dosing162 ± 21.49164 ± 22.4781.62 ± 5.020.50 ± 0.000.28 ± 0.00 2.41 ± 0.01
体外研究:
Amtolmetin guacil (100 μM; 0-60 min) converts to TMT (Tolmetin, HY-B1799) along with MED5 (1-methyl-5-p-methylbenzoyl-pyrrol-2-acetamido aceticacid) in rat fresh plasma and rat liver microsomal, rapidly converts to MED5 and MED5 methyl ester without yielding TMT in human fresh plasma and human liver microsomes.