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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Phosphodiesterase (PDE)-Orismilast
Orismilast

Chemical Structure : Orismilast

CAS No.: 1353546-86-7

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Orismilast (LEO-32731, LEO 32731)

货号: PC-49587Not For Human Use, Lab Use Only.

Orismilast (LEO-32731) is a potent, selective, second generation PDE4 inhibitor with IC50 values of 3-52 nM for PDE4A/4B/4D subtype splice variants.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    Orismilast (LEO-32731) is a potent, selective, second generation PDE4 inhibitor with IC50 values of 3-52 nM for PDE4A/4B/4D subtype splice variants.
    Orismilast (LEO-32731) potently inhibits all PDE4B and PDE4D subtype splice variants compared to apremilast and demonstrates reduced potency for the PDE4C2 subtype and PDE4A10 subtype compared to other PDE4 subtypes with an IC50 of approximately 104 nM and 52
    nM, respectively.
    Orismilast (LEO-32731) is a 5 times more potent inhibitor of LPS-induced TNFα release in PBMC (IC50=2 nM) and a 14 times more potent inhibitor of aCD3/aCD28 induced TNFα release in human whole blood.
    Orismilast (LEO-32731) inhibits the secretion of cytokines across all investigated T-helper cell sublineages, with most the profound effect on Th1-cell effector cytokines but also demonstrates potent inhibition on Th17 cells and Th2 cells related cytokines.
    Orismilast (LEO-32731) (10 mg/kg and 30 mg/kg, oral) significantly reduced ear thickness and inflammation markers in vivo in the murine chronic oxazolone mouse model.

    物理化学性质&存储条件

    分子量 510.29
    分子式 C19H15Cl2F2NO7S
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    2-(3,5-Dichloro-1-oxido-4-pyridinyl)-1-[7-(difluoromethoxy)-2′,3′,5′,6′-tetrahydro-1′,1′-dioxidospiro[1,3-benzodioxole-2,4′-[4H]thiopyran]-4-yl]ethanone

    参考文献

    1. Silverberg JI, et al. J Eur Acad Dermatol Venereol. 2022 Dec 17. doi: 10.1111/jdv.18818.

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