LEO 39652 is a dual-soft PDE4 inhibitor with IC50 values of 1.2 nM for PDE4A, 1.2 nM for PDE4B, 3.0 nM for PDE4C, and 3.8 nM for PDE4D. LEO 39652 also inhibits TNF-α with an IC50 value of 6.0 nM. LEO 39652 is used in topical studies of atopic dermatitis.
|Solubility (25°C)||DMSO : 25 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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ONO-8430506 is a potent autotaxin phosphodiesterase inhibitor with significant oral exposure and low clearance in higher species.
Compound BIO-32546 is a potent (IC50=1 nM), selective, orally administered, non-zinc-binding reversible inhibitor of autophagy (ATX).
Ro 20-1724 is a potent inhibitor of PDE IV with Ki value of 3.1 μM and a potent gastric secretagogues.
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