| Chemical Properties | Back Directory | [Boiling point ]
788.8±60.0 °C(Predicted) | [density ]
1.70±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
-0.68±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Orismilast (LEO-32731) is an orally active and selective PDE4 inhibitor used for the research of inflammatory diseases. Orismilast demonstrates potent inhibition of PDE4B and PDE4D subtype splice variants[1][2]. | [in vivo]
Orismilast (10 and 30mg/kg) significantly reduces ear thickness and inflammation markers (p<0.0001, respectively)[2]. | Animal Model: | Female BALB/cABomTac mice (sensitized to oxazolone on the right ear with a single application of 10 μl oxazolone (0.8% in acetone) on Day 7)[2]. | | Dosage: | 10 and 30mg/kg. | | Administration: | Orally. | | Result: | Both the 10 mg/kg and 30mg/kg doses of oral orismilast resulted in a significant reduction in ear thickness over time (p<0.0001, respectively;) with no impact on bodyweight during the treatment period. |
| [IC 50]
PDE4B3: 3 nM (IC50); PDE4D7: 3 nM (IC50); PDE4D5: 3 nM (IC50); PDE4B2: 6 nM (IC50); PDE4D3: 8 nM (IC50); PDE4D4: 8 nM (IC50); PDE4D1: 9 nM (IC50); PDE4D2: 9 nM (IC50); PDE4A4: 11 nM (IC50); PDE4B1: 16 nM (IC50); PDE4A1: 16 nM (IC50); PDE4A10: 52 nM (IC50); PDE4C2: 104 nM (IC50) | [storage]
Store at -20°C | [References]
[1] Nielsen,et al.Preparation of benzodioxole or benzodioxepine heterocyclic compounds as phosphodiesterase inhibitors.WO2011160632A1.
[2] Jonathan I Silverberg, et al. Pharmacology of orismilast, a potent and selective PDE4 inhibitor. J Eur Acad Dermatol Venereol. 2023 Apr;37(4):721-729. DOI:10.1111/jdv.18818 |
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