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.
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- CAS No.: 1584160-52-0
- 화학식: C27H38N6O5
- 분자량:526.63
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Hartley guinea pigs (3 weeks old at purchase, 5 weeks old at challenge); Ovalbumin (HY-W250978)-sensitized allergic rhinitis model[2]
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Dosage:1, 3, 10, 30, 60 mg/kg
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Administration:Oral administration; single dose 1 h before the 3rd challenge, or once daily for 15 days
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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.
Chemical Information
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CAS No. 1584160-52-0
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분자량 526.63
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화학식 C27H38N6O5
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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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Synonyms
TAS-205
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[2]. Aoyagi H, et al. Potential synergistic effects of novel hematopoietic prostaglandin D synthase inhibitor TAS-205 and different types of anti-allergic medicine on nasal obstruction in a Guinea pig model of experimental allergic rhinitis. Eur J Pharmacol. 2020 May 15;875:173030. [Content Brief]
[3]. Komaki H, et al. Early phase 2 trial of TAS-205 in patients with Duchenne muscular dystrophy. Ann Clin Transl Neurol. 2020 Feb;7(2):181-190. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pizuglanstat hydrate Related Classifications
HY-109134A Related Classifications
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