Pizuglanstat (TAS-205) | H-PGDS inhibitor

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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5 mg	$78	In stock
10 mg	$118	In stock
25 mg	$218	In stock
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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.

Pizuglanstat (TAS-205, TAS205)

Biological Activity

Physicochemical Properties

References

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