Product Introduction
Bioactivity


英文名: Aglafoline

描述: Aglafoline inhibits in a concentration-dependent manner the aggregation and ATP release reaction induced in washed rabbit platelets by PAF (platelet-activating factor). The IC50 values of Aglafoline on PAF (3.6 nM)-induced platelet aggregation were about 50 μM.

体外活性: Aglafoline also inhibits [3H]PAF (3.6 nM) binding to washed rabbit platelets (IC50: 17.8 μM). The concentration-response curve of PAF-induced platelet aggregation was shifted to the right by Aglafoline (pA2: 5.97; pA10: 5.04). Although thromboxane B2 formation caused by collagen and thrombin was partially suppressed by Aglafoline, thromboxane B2 formation caused by ionophore A23187 and arachidonic acid was not affected. Aglafoline inhibited the [3H]inositol monophosphate formation caused by PAF but not that caused by collagen or thrombin in the presence of indomethacin (20 μM).

体内活性: The cAMP content of washed rabbit platelets was not affected by Aglafoline. Rat femoral intravenous administration of Aglafoline (10 mg/kg) did not affect blood pressure. However, Aglafoline (10 mg/kg) both prophylactically and therapeutically antagonized PAF (2.5 μg/kg)-induced hypotensive shock in rats. Intravenous PAF (30 ng/kg) caused severe bronchoconstriction in guinea pigs. This effect was completely blocked by Aglafoline.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 100 mg/mL (203.04 mM)
DMSO : 21.43 mg/mL (43.51 mM)


关键字: Aglafoline | Methyl rocaglate