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.
| Molecular Weight | 421.45 |
| Formula | C23H23N3O5 |
| CAS Number | 1445656-91-6 |
| Solubility (25°C) | DMSO : 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| 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.
| Related PDE Products |
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| N-Methylbenzylamine
N-Methylbenzylamine, a small molecule inhibitor targeting phosphodiesterase-5 (PDE-5), exerts neuroprotective effects by inhibiting neuronal apoptosis and restoring synaptic plasticity, and can be used in studies related to Alzheimer's disease (AD). |
| Kushenol B
Kushenol B is an isoprenoid flavonoid isolated from S. flavescens, has antimicrobial, anti-inflammatory and antioxidant activities. Kushenol B has inhibitory activity against cAMP phosphodiesterase (PDE), with an IC50 of 31 µM. |
| Mangostanol
Mangostanol ((+)-Mangostanol) is a polyoxygenated xanthone mangostanol, which can be isolated from the shell of Garcinia mangostana, and has inhibitory effect on cAMP phosphodiesterase (PDE). |
| N-Desmethyl Sildenafil
N-Desmethyl Sildenafil (Desmethylsildenafil) is a major metabolite of Sildenafil. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor. |
| 5,7-Diacetoxy-8-methoxyflavone
5,7-Diacetoxy-8-methoxyflavone is a natural product that could come from scutellaria genus plants. 5,7-Diacetoxy-8-methoxyflavone has inhibitory activity for cAMP phosphodiesterase. |
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