Cas No.: | 1273323-67-3 |
Chemical Name: | YLF-466D |
Synonyms: | YLF-466D;C24;YLF 466D |
SMILES: | O=C(O)C1=CC=CC(CN2C(/C(C3=C2C=CC=C3)=C(C4=CC=C(Cl)C=C4)\C5=CC=CC=C5)=O)=C1 |
Formula: | C29H20ClNO3 |
M.Wt: | 465.927006721497 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Target: | AMPK |
In Vitro: | 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]. |
Kinase Assay: | 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]. |
References: | [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. |