产品
编 号：F504592
分子式：C23H11ClN4
分子量：378.81
分子式：C23H11ClN4
分子量：378.81
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
询价
50mg
询价
询价
结构图
CAS No: 892549-43-8
产品详情
生物活性：
MF63 is a selective and orally active inhibitor of mPGES-1. MF63 reduces the accumulation of PGE2, relieves pyresis, hyperalgesia, and inflammatory pain by inhibiting mPGES-1.
体内研究：
MF63 (100 mg/kg；口服；单剂量) 可减少 KI (敲入 mPGES-1 基因) 小鼠气囊和大脑中 PEG2 的积累，并以剂量依赖的方式抑制 PEG2 的形成。MF63 (10 mg/kg 和 100 mg/kg；口服；单剂量) 以剂量依赖的方式抑制 KI 小鼠中 LPS 诱导的痛觉过敏反应。MF63 (0-150 mg/kg；口服；单剂量) 抑制豚鼠中 PEG2 合成、痛觉过敏、发热，并缓解慢性骨关节炎样疼痛。MF63 (0-100 mg/kg；口服；每天两次，共 4 天) 对 KI 小鼠和非人类灵长类动物具有胃肠耐受性。Animal Model:10 to 12 weeks of KI and wild-type mice which injected LPS.
Dosage:10 mg/kg and 100 mg/kg.
Administration:Oral gavage; single dose.
Result:Inhibited the PGE2 accumulation in air pouch and brain of KI mice in a dose-dependent manner, and has selectively in the brain. Reduced the response of hyperalgesia by 50% at 10 mg/kg and 80% at 100 mg/kg in KI mice but without effecting wild-type mice.
Animal Model:Young male Hartley guinea pigs (~250 g) with osteoarthritic pain.
Dosage:0, 3, 10, 15, 30, 50, 100 or 150 mg/kg.
Administration:Oral gavage; single dose.
Result:Inhibited the formation of PGE2 in a dose-dependent manner, relieved Chronic Osteoarthritic-Like Pain and also inhibited pyresis.
Animal Model:10 to 12 weeks of KI mice and nonhuman primates.
Dosage:0, 3, 10, 30 or 100 mg/kg.
Administration:Oral gavage; twice daily for 4 days.
Result:Had no gastrointestinal toxicity in KI mice and non-human primates.
体外研究：
MF63 (0.01-100 μM；24 h) 选择性抑制 A549 细胞中 10 ng/mL IL-1β 诱导的 PGE2 生成，并以剂量依赖的方式增加 PGF2α 的形成。MF63 (10 μM；24 h) 增强了多种金属硫蛋白 1 (MT1) 亚型以及 IL-1 和 IL-36 的内源性拮抗剂的表达，具有抗炎作用。
MF63 is a selective and orally active inhibitor of mPGES-1. MF63 reduces the accumulation of PGE2, relieves pyresis, hyperalgesia, and inflammatory pain by inhibiting mPGES-1.
体内研究：
MF63 (100 mg/kg；口服；单剂量) 可减少 KI (敲入 mPGES-1 基因) 小鼠气囊和大脑中 PEG2 的积累，并以剂量依赖的方式抑制 PEG2 的形成。MF63 (10 mg/kg 和 100 mg/kg；口服；单剂量) 以剂量依赖的方式抑制 KI 小鼠中 LPS 诱导的痛觉过敏反应。MF63 (0-150 mg/kg；口服；单剂量) 抑制豚鼠中 PEG2 合成、痛觉过敏、发热，并缓解慢性骨关节炎样疼痛。MF63 (0-100 mg/kg；口服；每天两次，共 4 天) 对 KI 小鼠和非人类灵长类动物具有胃肠耐受性。Animal Model:10 to 12 weeks of KI and wild-type mice which injected LPS.
Dosage:10 mg/kg and 100 mg/kg.
Administration:Oral gavage; single dose.
Result:Inhibited the PGE2 accumulation in air pouch and brain of KI mice in a dose-dependent manner, and has selectively in the brain. Reduced the response of hyperalgesia by 50% at 10 mg/kg and 80% at 100 mg/kg in KI mice but without effecting wild-type mice.
Animal Model:Young male Hartley guinea pigs (~250 g) with osteoarthritic pain.
Dosage:0, 3, 10, 15, 30, 50, 100 or 150 mg/kg.
Administration:Oral gavage; single dose.
Result:Inhibited the formation of PGE2 in a dose-dependent manner, relieved Chronic Osteoarthritic-Like Pain and also inhibited pyresis.
Animal Model:10 to 12 weeks of KI mice and nonhuman primates.
Dosage:0, 3, 10, 30 or 100 mg/kg.
Administration:Oral gavage; twice daily for 4 days.
Result:Had no gastrointestinal toxicity in KI mice and non-human primates.
体外研究：
MF63 (0.01-100 μM；24 h) 选择性抑制 A549 细胞中 10 ng/mL IL-1β 诱导的 PGE2 生成，并以剂量依赖的方式增加 PGF2α 的形成。MF63 (10 μM；24 h) 增强了多种金属硫蛋白 1 (MT1) 亚型以及 IL-1 和 IL-36 的内源性拮抗剂的表达，具有抗炎作用。
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备