Orismilast

• CAT Number: I030638
• CAS Number: 1353546-86-7
• Molecular Formula: C19H15Cl2F2NO7S
• Molecular Weight: 510.29
• Purity: ≥95%
• Synonyms: 2-(3,5-dichloro-1-oxidopyridin-1-ium-4-yl)-1-[7-(difluoromethoxy)-1′,1′-dioxospiro[1,3-benzodioxole-2,4′-thiane]-4-yl]ethanone
• InChI: InChI=1S/C19H15Cl2F2NO7S/c20-12-8-24(26)9-13(21)11(12)7-14(25)10-1-2-15(29-18(22)23)17-16(10)30-19(31-17)3-5-32(27,28)6-4-19/h1-2,8-9,18H,3-7H2
• InChIKey: ZININGNRPUGNSL-UHFFFAOYSA-N
• SMILES: C1CS(=O)(=O)CCC12OC3=C(C=CC(=C3O2)OC(F)F)C(=O)CC4=C(C=[N+](C=C4Cl)[O-])Cl

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].
Orismilast inhibits tumour necrosis factor α (TNFα), and the secretion of T-helper (Th)1 (TNFα and IFNγ), Th17 (IL-22 and IL-23), and Th2 (IL-4, IL-5, and IL-13) related cytokines in PBMC[2].
Orismilast (10 and 30mg/kg) significantly reduces ear thickness and inflammation markers (p<0.0001, respectively)[2].

Reference

[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.
 [Content Brief]