YLF-466D

An AMPK activator

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2mg

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货号: ajci20658
CAS: 1273323-67-3
别名: 3-[[(3E)-3-[(4-氯苯基)苯基亚甲基]-2,3-二氢-2-氧代-1H-吲哚-1-基]甲基]苯甲酸,C24
分子式: C29H20ClNO3
分子量: 465.9
纯度: >98%
溶解度: DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml,Ethanol: 10 mg/ml
储存: Store at -20°C
库存: 现货

Background

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].

参考文献:
[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.

Protocol

Kinase experiment:

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].

参考文献:

[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.