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Product details

名称

Timapiprant sodium

别名

替马匹兰钠

英文名称

Timapiprant sodium

货号

T646129-5mg

包装规格

5mg

浓度

≥99%

储存温度

2-8°C储存

运输条件

冰袋运输

产品介绍

Timapiprant sodium (OC000459 sodium) is a potent, selective, and orally active D prostanoid receptor 2 ( DP 2 , also known as CRTH2 ) antagonist. Timapiprant sodium (OC000459 sodium) potently displaces [ 3 H] PGD2 from human recombinant DP 2 ( K i =13 nM), rat recombinant DP 2 ( K i =3 nM), and human native DP 2 ( K i =4 nM). Timapiprant sodium (OC000459 sodium) inhibits mast cell activation of Th2 lymphocytes and eosinophils In Vitro Timapiprant sodium (OC000459 sodium) (0.0001 μM-10 μM; 5 hours) inhibits chemotaxis (IC 50 =0.028 μM) of human Th2 lymphocytes and cytokine production (IC 50 =0.019 μM) by human Th2 lymphocytes. Timapiprant sodium (OC000459 sodium) (1 μM) inhibits the activation of Th2 cells and eosinophils in response to supernatants from IgE/anti-IgE-activated human mast cells. Timapiprant sodium (OC000459 sodium) (1 nM-1000 nM; 16 hours) inhibits the anti-apoptotic effect of PGD2 on Th2 cells with an IC 50 of 0.035 uM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis AnalysisCell Line: Th2 Cells Concentration: 0.0001 μM-10 μM Incubation Time: 16 hours Result: Inhibited the antiapoptotic effect of PGD2. In Vivo Timapiprant sodium (OC000459 sodium) (gavage; 2 mg/kg, 10 mg/kg) inhibits blood eosinophilia induced by 13,14-dihydro-15-keto-PGD2 (DK-PGD2) in Rat (ED 50 =0.04 mg/kg) . Timapiprant sodium (OC000459 sodium) (gavage; 0.01 mg/kg, 0.1 mg/kg, 1.0 mg/kg) inhibits airway eosinophilia in response to an aerosol of DK-PGD2 in guinea pigs (ED 50 =0.01 mg/kg) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:Ki: 0.013 μM (human recombinant DP2),0.003 μM (rat recombinant DP2) and 0.004 μM (human native DP2)

生化机理

替马扑仑钠（OC000459 sodium）是一种强效、选择性和口服活性的 D 类前列腺素受体 2（DP 2，又称 CRTH2）拮抗剂。替马扑仑钠（OC000459 钠）能强效置换人重组 DP 2 中的 [ 3 H] PGD2（K i =13 nM）。

CAS号

950688-14-9

分子式

C21H16FN2NaO2

分子量

370.35 g/mol

Smiles

O=C(O[Na])CN1C2=CC=C(F)C=C2C(CC3=NC4=C(C=CC=C4)C=C3)=C1C

溶解性

DMSO : 100 mg/mL (270.01 mM; Need ultrasonic)

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

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