1. GPCR/G Protein
  2. Platelet-activating Factor Receptor (PAFR)
  3. YM-264

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。

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YM-264 Chemical Structure

YM-264 Chemical Structure

CAS No. : 131888-54-5

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规格 价格 是否有货 数量
1 mg ¥2300
2 - 4 周
5 mg ¥6000
2 - 4 周
10 mg 现货 2 - 4 周
25 mg 现货 2 - 4 周
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Customer Review

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

YM-264 is a selective, potent and orally active platelet-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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

540.67

Formula

C28H36N4O5S

CAS 号
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.

纯度 & 产品资料
参考文献
Animal Administration
[2]

Guine Pigs[2]
Male Hartley guinea pigs weighing approximately 300 g are sensitized. The animals are fixed in position with the nose and mouth directed toward the center of the cylinder. Ovalbumin (10 mg/mL) is administered daily for 10 min. On the ninth or tenth day, all of the animals exhibit asthmatic symptoms. Two booster inhalations of AO (10 mg/mL) are subsequently given to the guinea pigs for 5 min at weekly intervals. Forty-five animals are randomized into three experimental groups by the order of their capture from shipping crate. Each group is further divided into three subgroups for control, YM-264 (1 mg/kg) and YM-264 (3 mg/kg). One week after the second booster inhalation, 16 animals for AH experiment are randomly divided into three subgroups for control and YM-264 treatment (1 and 3 mg/kg), and they are exposed to aerosolized OA (10 mg/mL) for 5 min. A dose of 1 or 3 mg/kg of YM264 is administered orally 30 min before and again, 3 h after the exposure to OA. The control group receives 0.5% methylcellulose in the same volume as YM-264[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
YM-264
目录号:
HY-101833
需求量: