YLF-466D

Names

[ CAS No. ]:
1273323-67-3

[ Name ]:
YLF-466D

[Synonym ]:
(E)-3-((3-((4-chlorophenyl)(phenyl)methylene)-2-oxoindolin-1-yl)methyl)benzoic acid
3-{3-[1-(4-chloro-phenyl)-1-phenyl-meth-(E)-ylidene]-2-oxo-2,3-dihydro-indol-1-ylmethyl}-benzoic acid
3-{3-[1-(4-chlorophenyl)-1-phenylmeth-(E)-ylidene]-2-oxo-2,3-dihydroindol-1-ylmethyl}-benzoic acid
3-((3-((4-chlorophenyl)(phenyl)meth-(E)-ylene)-2-oxoindolin-1-yl)methyl)benzoic acid
YLF-466D

Biological Activity

[Description]:

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

[Related Catalog]:

Signaling Pathways >> Epigenetics >> AMPK
Signaling Pathways >> PI3K/Akt/mTOR >> AMPK
Research Areas >> Cancer

[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.


[Related Small Molecules]

Dorsomorphin dihydrochloride | Acadesine (AICAR) | A-769662 | Phenformin (hydrochloride) | Bempedoic Acid | Flufenamic Acid | WZ 4003 | PF 06409577 | Dantron | O-304 | 6-Gingerol | 7-Methoxyisoflavone | HTH 01-015 | Ampkinone

Chemical & Physical Properties

[ Molecular Formula ]:
C29H20ClNO3

[ Molecular Weight ]:
465.92700

[ Exact Mass ]:
465.11300

[ PSA ]:
57.61000

[ LogP ]:
6.60910

[ Storage condition ]:
2-8℃

Related Compounds