Timapiprant,950688-14-9

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Timapiprant sodium

CAS No. : 950688-14-9

MCE 国际站：Timapiprant sodium

产品活性：Timapiprant sodium (OC000459 sodium) 是一种高效选择性的口服型 D 前列腺素受体 2 (DP₂，也称为 CRTH2) 拮抗剂。Timapiprant sodium (OC000459 sodium) 有效地置换来自人重组 DP₂ (K _i=13 nM)，大鼠重组 DP₂ ( K _i=3 nM) 和人天然 DP₂ ( K _i=4 nM) 的 [³H] PGD2。 Timapiprant sodium (OC000459 sodium) 抑制肥大细胞激活 Th2 淋巴细胞和嗜酸性粒细胞。

研究领域：GPCR/G Protein

作用靶点：Prostaglandin Receptor

In Vitro: Timapiprant sodium (OC000459 sodium) (0.0001 μM-10 μM; 5 hours) inhibits chemotaxis (IC₅₀=0.028 μM) of human Th2 lymphocytes and cytokine production (IC₅₀=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 IC₅₀ of 0.035 uM.

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 (ED₅₀=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 (ED₅₀=0.01 mg/kg).

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