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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.70%
- CAS 番号: 1244967-98-3
- 分子式: C27H36N6O4
- 分子量:508.61
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保管条件: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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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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 |
化学情報
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CAS 番号 1244967-98-3
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性状 Solid
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分子量 508.61
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分子式 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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別名
TAS-205 free base
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (272 KB)
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SDS (254 KB)
- English - EN (254 KB)
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- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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取扱説明書 (2659 KB)
参考文献
[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 |
|---|---|---|---|---|---|
| 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 関連分類
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