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Pizuglanstat

Chemical Structure : Pizuglanstat

CAS No.: 1244967-98-3

Pizuglanstat (TAS-205, TAS205)

Catalog No.: PC-36096Not 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, 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.
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 508.623
Formula C27H36N6O4
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-pyrrole-2-carbonyl)-N-{4-[4-(morpholine-4-carbonyl)piperidin-1-yl]phenyl}piperazine-1-carboxamide

References

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

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