2. GPCR/G Protein
  3. Prostaglandin Receptor
  4. Pizuglanstat

Pizuglanstat  (Synonyms: TAS-205 free base)

製品番号: HY-109134 純度: 99.70%
COA 取扱説明書 Technical Support

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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Pizuglanstat

Pizuglanstat 構造式

CAS 番号 : 1244967-98-3

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 62 在庫あり
Solution
10 mM * 1 mL in DMSO USD 62 在庫あり
Solid
5 mg $55 在庫あり
10 mg $90 在庫あり
25 mg $195 在庫あり
50 mg $285 在庫あり
100 mg $410 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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製品説明

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[1][2][3].

IC50 & Target

DP

 

体外実験

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.

Pizuglanstat 関連抗体
体内実験

Pizuglanstat (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.
臨床実験
分子量

508.61

分子式

C27H36N6O4
CAS 番号
Appearance

Solid

Color

White to light yellow

SMILES

O=C(N1CCOCC1)C2CCN(C3=CC=C(NC(N4CCN(C(C5=CC=CN5C)=O)CC4)=O)C=C3)CC2
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9661 mL 9.8307 mL 19.6614 mL
5 mM 0.3932 mL 1.9661 mL 3.9323 mL
10 mM 0.1966 mL 0.9831 mL 1.9661 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

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体積 （終了）

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
純度とドキュメンテーション

純度: 99.70%

COA (247 KB) LCMS (94 KB)

取扱説明書 (2659 KB)
参考文献

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
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Pizuglanstat Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

Pizuglanstat1244967-98-3TAS-205TAS205TAS 205Prostaglandin Receptorallergic rhinitisguinea pigsRBL-2H3KU812Inhibitorinhibitorinhibit

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製品番号:
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