YLF-466D is a newly developed AMPK activator, which inhibits platelet aggregation.

The effect of YLF-466D on platelet AMPK and aggregation are examined to test whether YLF-466D can stimulate AMPK in platelets and thereby suppress aggregation. Platelet AMPK is activated by YLF-466D, which is confirmed with activation-dependent phosphorylation at Thr172. Consistent with this result, YLF-466D inhibits platelet aggregation induced by thrombin. Such inhibition is observed in the aggregation elicited by ADP and collagen as well as thrombin, indicating that the antiaggregatory effect of YLF-466D is not platelet-agonist specific but common, regardless of agonist type. All the effects on AMPK and aggregation are concentration-dependent with the highest efficacy at 150 μM. IC₅₀ against thrombin-, ADP- and collagen-induced aggreation are approximately 84, 55 and 87 μM, respectively^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

465.93

C₂₉H₂₀ClNO₃

1273323-67-3

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : ≥ 100 mg/mL (214.62 mM)

* “≥” means soluble, but saturation unknown.

*

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• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.5 mg/mL (5.37 mM); Clear solution

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  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

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• 2.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.5 mg/mL (5.37 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (5.37 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Liu Y, et al. Antiplatelet effect of a newly developed AMP-activated protein kinase activator YLF-466D. Eur J Pharmacol. 2015 Aug 5;760:81-7.

Blood is collected from the abdominal aorta of ether anesthetized rats using 3.2% sodium citrate as an anticoagulant (sodium citrate:blood=1:9) and diluted with normal saline (1:1). Blood is incubated with YLF-466D (0, 50, 100 and 150 μM) for 3 min and aggregation is induced with 7.5 μg/mL Collagen. Aggregation is assessed by measuring the impedance change with a whole blood aggregometer^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Liu Y, et al. Antiplatelet effect of a newly developed AMP-activated protein kinase activator YLF-466D. Eur J Pharmacol. 2015 Aug 5;760:81-7.