TAS-205 (Pizuglanstat) monohydrate | H-PGDS inhibitor

Chemical Structure : TAS-205 monohydrate

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TAS-205 monohydrate (Pizuglanstat)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	526.64
分子式	C27H38N6O5
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	4-[(1-methyl-1H-pyrrol-2-yl)carbonyl]-N-[4-[4-(4-morpholinylcarbonyl)-1-piperidinyl] phenyl]-1-piperazinecarboxamide monohydrate

参考文献

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

TAS-205 monohydrate (Pizuglanstat)

生物&药学活性

物理化学性质&存储条件

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TAS-205 monohydrate (Pizuglanstat)

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物理化学性质&存储条件

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