LEO 39652

LEO 39652 is a dual-soft PDE4 inhibitor with IC 50 s 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 IC 50 value of 6.0 nM. LEO 39652 is used for topical research of Atopic dermatitis (AD) In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo LEO 39652 is inactivated both in blood and liver (dual-soft) while stabled in the skin . Pharmacokinetic Analysis LEO 39652 exhibits total clearance (rats 930, minipigs 200 and monkey 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) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 3 male Sprague Dawley rats, 2 female Göttingen minipigs, 2 male Göttingen 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. Form:Solid IC50& Target:PDE4D 3.8 nM (IC 50 ) TNF-α 6.0 nM (IC 50 ) PDE4A 1.2 nM (IC 50 ) PDE4B 1.2 nM (IC 50 ) PDE4C2 3.0 nM (IC 50 )

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