1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. Pizuglanstat hydrate

Pizuglanstat hydrate (Compound 3; TAS-205) is an orally active prostaglandin D synthase inhibitor with an IC50 of 76 nM for human hematopoietic prostaglandin D synthase. Pizuglanstat hydrate inhibits the synthesis of PGD2. Pizuglanstat hydrate improves experimental allergic rhinitis. Pizuglanstat hydrate can be used in the study of muscle regenerative diseases such as muscular dystrophy.

For research use only. We do not sell to patients.

Pizuglanstat hydrate Chemical Structure

Pizuglanstat hydrate Chemical Structure

CAS No. : 1584160-52-0

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Description

Pizuglanstat hydrate (Compound 3; TAS-205) is an orally active prostaglandin D synthase inhibitor with an IC50 of 76 nM for human hematopoietic prostaglandin D synthase. Pizuglanstat hydrate inhibits the synthesis of PGD2. Pizuglanstat hydrate improves experimental allergic rhinitis. Pizuglanstat hydrate can be used in the study of muscle regenerative diseases such as muscular dystrophy[1][2][3].

In Vitro

Pizuglanstat hydrate (10-3000 nM) inhibits PGD2 synthesis in basophilic cells (RBL-2H3 and KU812)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Pizuglanstat hydrate (1-60 mg/kg; p.o.; single dose or once daily for 15 days) suppresses late-phase nasal obstruction, eosinophil infiltration, and PGD2 production in nasal lavage fluid in a guinea pig model of experimental allergic rhinitis[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Hartley guinea pigs (3 weeks old at purchase, 5 weeks old at challenge); Ovalbumin (HY-W250978)-sensitized allergic rhinitis model[2]
Dosage: 1, 3, 10, 30, 60 mg/kg
Administration: Oral administration; single dose 1 h before the 3rd challenge, or once daily for 15 days
Result: Dose-dependently reduced PGD2 levels in nasal lavage fluid, suppressed late-phase nasal obstruction (area under the curve of specific airway resistance from 3-7 h).
Inhibited eosinophil infiltration into the nasal cavity.
Had additive effects on eosinophil suppression and late-phase obstruction when used in combination with Montelukast (HY-13315A), and when used in combination with Fexofenadine (HY-B0801), the suppression of early and late-phase obstruction is comparable to monotherapy.
Molecular Weight

526.63

Formula

C27H38N6O5

CAS No.
SMILES

O=C(N1CCOCC1)C2CCN(C3=CC=C(NC(N4CCN(C(C5=CC=CN5C)=O)CC4)=O)C=C3)CC2.O

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Pizuglanstat hydrate
Cat. No.:
HY-109134A
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