Pizuglanstat
Based on 1 Customer Validation
Pizuglanstat (Compound 3; TAS-205 free base) is an orally active prostaglandin D synthase inhibitor with an IC50 of 76 nM for human hematopoietic prostaglandin D synthase. Pizuglanstat inhibits the synthesis of PGD2. Pizuglanstat improves experimental allergic rhinitis. Pizuglanstat can be used in the study of muscle regenerative diseases such as muscular dystrophy.
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- Purity: 99.70%
- CAS No.: 1244967-98-3
- 화학식: C27H36N6O4
- 분자량:508.61
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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DP |
Pizuglanstat (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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1244967-98-3
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Appearance Solid
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분자량 508.61
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화학식 C27H36N6O4
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Color White to light yellow
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SMILES
O=C(N1CCOCC1)C2CCN(C3=CC=C(NC(N4CCN(C(C5=CC=CN5C)=O)CC4)=O)C=C3)CC2
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Synonyms
TAS-205 free base
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 12.5 mg/mL (24.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (272 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.9661 mL | 9.8307 mL | 19.6614 mL | 49.1536 mL |
| 5 mM | 0.3932 mL | 1.9661 mL | 3.9323 mL | 9.8307 mL | |
| 10 mM | 0.1966 mL | 0.9831 mL | 1.9661 mL | 4.9154 mL | |
| 15 mM | 0.1311 mL | 0.6554 mL | 1.3108 mL | 3.2769 mL | |
| 20 mM | 0.0983 mL | 0.4915 mL | 0.9831 mL | 2.4577 mL |
Pizuglanstat Related Classifications
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