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YM-264
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
YM-264图片
CAS NO:131888-54-5
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
YM-264 是一种有口服活性的、血小板活化因子 (PAF)的有效选择性拮抗剂,其在兔子血小板膜上的 pKi值为 8.85。
生物活性

YM-264 is a selective, potent and orally activeplatelet-activating factor (PAF)antagonist with a pKi value of 8.85 for rabbit platelet membranes.

IC50& Target

pKi: 8.85 (PAF, rabbit platelet membranes)[1].

体外研究
(In Vitro)

The anti-platelet-activating factor effect of YM-264 is examined in vitro. YM-264 inhibits [3H] platelet-activating factor binding to rabbit platelet membranes with a pKivalue of 8.85. YM-264 inhibits the platelet-activating factor-induced human, rabbit and guinea-pig platelet aggregation with pA2 values of 8.68, 8.33 and 8.14, respectively[1].

体内研究
(In Vivo)

There are no significant differences in baseline airway responsiveness between control and YM-264 treated groups. Airway hyperresponsiveness induced by antigen exposure is significantly inhibited by the administration of YM-264. The baseline Rrs is 0.40 (0.02) cm H2O/mL/s in the control group (n=6). In the YM-264 treated groups, the baseline Rrs is 0.39 (0.01) and 0.36 (0.01) cm H2O/mL/s at a doses of 1 mg/kg (n=5) and 3 mg/kg (n=6), respectively. The Rrs during the IAR significantly increase from baseline to 0.92 (0.10) cm H2O/mL/s in control (p=0.0002), 0.81 (0.12) in YM-264 1 mg/kg (p=0.01), and 1.06 (0.29) in YM-264 3 mg/kg (p=0.048). Reelevation of Rrs in the late phase is observed in the control group after antigen challenge. At this phase, Rrs significantly increase to 0.72 (0.10) cm H2O/mL/s (p=0.0101) from the baseline (0.40) at 6 h after the exposure of antigen. In contrast, YM-264 at the doses of 1 and 3 mg/kg show significant inhibition of reelevation of Rrs as compared with control. YM-264 inhibit the eosinophil infiltration dose dependently[2].

分子量

540.67

Formula

C28H36N4O5S

CAS 号

131888-54-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.