Timapiprant sodium - ≥99% , CAS No.950688-14-9

CAS: 950688-14-9 Cat. No.: T646129 Fórmula: C₂₁H₁₆FN₂NaO₂ Peso molecular: 370.35

GRADE & PURITY ≥99%

Storage

Store at 2-8°C

Shipped In

Wet ice

Descripción general

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)

Specifications

Especificaciones y pureza

≥99%

Mecanismos bioquímicos y fisiológicos

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)

Condiciones de almacenamiento de almacenamiento

Store at 2-8°C

Enviado en

Wet ice

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Pureza

≥99%

Nombres e identificadores

• Sonrisas canónicas: O=C(O[Na])CN1C2=CC=C(F)C=C2C(CC3=NC4=C(C=CC=C4)C=C3)=C1C
• Peso molecular: 370.35

Propiedades químicas y físicas

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