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TAS-205 monohydrate

Chemical Structure : TAS-205 monohydrate

CAS No.: 1584160-52-0

TAS-205 monohydrate (Pizuglanstat)

Catalog No.: PC-49641Not For Human Use, Lab Use Only.

TAS-205 (Pizuglanstat, TAS205) is a potent, specific hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with IC50 of 55.8 nM, does not inhibit LPGDS at 100 uM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    TAS-205 (Pizuglanstat) monohydrate is a potent, specific hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with IC50 of 55.8 nM, does not inhibit LPGDS at 100 uM.
    TAS-205 did not affect the activities of 174 enzymes, including 10 arachidonic acid-related enzymes such as cyclooxygenase (COX)-1, COX-2, and LTC4 synthase or the binding of 164 receptors.
    TAS-205 inhibited PGD2 increase of calcium ionophore A23187-stimulated rat basophilic RBL-2H3 cells and human basophilic KU812 cells with IC50 of 181.3 nM and 78.3 nM, respectively, TAS-205 inhibited PGD2 production induced by the cross-linking of IgE on RBL-2H3 cells with IC50 of 238.4 nM.
    TAS-205 (30 mg/kg, p.o.) suppressed late phase nasal obstruction in our guinea pig model, TAS-205 alone and in combination with montelukast showed inhibitory effects on eosinophil infiltration into the nasal cavity.

    Physicochemical Properties

    M.Wt 526.64
    Formula C27H38N6O5
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    4-[(1-methyl-1H-pyrrol-2-yl)carbonyl]-N-[4-[4-(4-morpholinylcarbonyl)-1-piperidinyl] phenyl]-1-piperazinecarboxamide monohydrate

    References

    1. Aoyagi H, et al. Eur J Pharmacol. 2020 May 15;875:173030.

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