产品
编 号：F745253
分子式：C23H23N3O5
分子量：421.45
分子式：C23H23N3O5
分子量：421.45
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
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5mg
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10mg
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结构图
CAS No: 1445656-91-6
产品详情
生物活性：
LEO 39652 is a dual-soft PDE4 inhibitor with IC50s of 1.2 nM, 1.2 nM, 3.0 nM and 3.8 nM for PDE4A, PDE4B, PDE4C and PDE4D, respectively. LEO 39652 also inhibits TNF-α with an IC50 value of 6.0 nM. LEO 39652 is used for topical research of Atopic dermatitis (AD) .
体内研究：
LEO 39652 is inactivated both in blood and liver (dual-soft) while stabled in the skin.Pharmacokinetic AnalysisLEO 39652 exhibits total clearance (rats 930, minipigs 200 andmonkey 300 mL/min/kg) and ratio to total AUC (rats 4, minipigs 6 and monkey 6 %) following intravenous administration (rats 0.075, minipigs 0.5 and monkeys 2.0 mg/kg).Animal Model:3 male Sprague Dawley rats, 2 female Go?ttingen minipigs, 2 male Go?ttingen minipigs, 2 female cynomolgus monkeys and 2 male cynomolgus monkeys
Dosage:Rats 0.075, minipigs 0.5 and monkeys 2.0 mg/kg
Administration:Intravenous injection
Result:Total clearance of 930, 200 and 300 mL/min/kg for rats, minipigs and monkeys, respectively.
体外研究：
LEO 39652 shows unbound in vitro potency when measured as LPS induced TNF-α release in human peripheral blood mononuclear cells (PBMC), incubated in serum free medium. LEO 39652 shows a relatively high binding to human serum albumin.
LEO 39652 is a dual-soft PDE4 inhibitor with IC50s of 1.2 nM, 1.2 nM, 3.0 nM and 3.8 nM for PDE4A, PDE4B, PDE4C and PDE4D, respectively. LEO 39652 also inhibits TNF-α with an IC50 value of 6.0 nM. LEO 39652 is used for topical research of Atopic dermatitis (AD) .
体内研究：
LEO 39652 is inactivated both in blood and liver (dual-soft) while stabled in the skin.Pharmacokinetic AnalysisLEO 39652 exhibits total clearance (rats 930, minipigs 200 andmonkey 300 mL/min/kg) and ratio to total AUC (rats 4, minipigs 6 and monkey 6 %) following intravenous administration (rats 0.075, minipigs 0.5 and monkeys 2.0 mg/kg).Animal Model:3 male Sprague Dawley rats, 2 female Go?ttingen minipigs, 2 male Go?ttingen minipigs, 2 female cynomolgus monkeys and 2 male cynomolgus monkeys
Dosage:Rats 0.075, minipigs 0.5 and monkeys 2.0 mg/kg
Administration:Intravenous injection
Result:Total clearance of 930, 200 and 300 mL/min/kg for rats, minipigs and monkeys, respectively.
体外研究：
LEO 39652 shows unbound in vitro potency when measured as LPS induced TNF-α release in human peripheral blood mononuclear cells (PBMC), incubated in serum free medium. LEO 39652 shows a relatively high binding to human serum albumin.
产品资料
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