YLF-466D

CAS# 1273323-67-3

YLF-466D

Catalog No. BCC4086----Order now to get a substantial discount!

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Chemical structure

YLF-466D

3D structure

Chemical Properties of YLF-466D

Cas No. 1273323-67-3 SDF Download SDF
PubChem ID 51033997 Appearance Powder
Formula C29H20ClNO3 M.Wt 465.93
Type of Compound N/A Storage Desiccate at -20°C
Synonyms C24
Solubility DMSO : ≥ 100 mg/mL (214.62 mM)
H2O : < 0.1 mg/mL (insoluble)
*"≥" means soluble, but saturation unknown.
Chemical Name 3-[[(3E)-3-[(4-chlorophenyl)-phenylmethylidene]-2-oxoindol-1-yl]methyl]benzoic acid
SMILES C1=CC=C(C=C1)C(=C2C3=CC=CC=C3N(C2=O)CC4=CC=CC(=C4)C(=O)O)C5=CC=C(C=C5)Cl
Standard InChIKey BPBOVHROVFJFAH-CYYJNZCTSA-N
Standard InChI InChI=1S/C29H20ClNO3/c30-23-15-13-21(14-16-23)26(20-8-2-1-3-9-20)27-24-11-4-5-12-25(24)31(28(27)32)18-19-7-6-10-22(17-19)29(33)34/h1-17H,18H2,(H,33,34)/b27-26+
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of YLF-466D

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

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.

Protocol

Kinase Assay [1]
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.

YLF-466D Dilution Calculator

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Preparing Stock Solutions of YLF-466D

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.1462 mL 10.7312 mL 21.4625 mL 42.9249 mL 53.6561 mL
5 mM 0.4292 mL 2.1462 mL 4.2925 mL 8.585 mL 10.7312 mL
10 mM 0.2146 mL 1.0731 mL 2.1462 mL 4.2925 mL 5.3656 mL
50 mM 0.0429 mL 0.2146 mL 0.4292 mL 0.8585 mL 1.0731 mL
100 mM 0.0215 mL 0.1073 mL 0.2146 mL 0.4292 mL 0.5366 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on YLF-466D

YLF-466D is an allosteric AMPK activator.

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References on YLF-466D

Antiplatelet effect of a newly developed AMP-activated protein kinase activator YLF-466D.[Pubmed:25913239]

Eur J Pharmacol. 2015 Aug 5;760:81-7.

AMP-activated protein kinase (AMPK) acts as a major regulator of cellular energy homeostasis. In platelets, AMPK activation stimulates endothelial nitric oxide synthase (eNOS) and its downstream signaling, and thereby inhibits platelet aggregation. In this study, a newly developed AMPK activator 3-[[(3E)-3-[(4-chlorophenyl)phenylmethylene]-2,3-dihydro-2-oxo-1H-indol-1-yl]meth yl]-benzoic acid (YLF-466D) was tested for its antiplatelet activity. Treatment of isolated platelets with YLF-466D resulted in AMPK activation in a concentration-dependent manner in a range of 50-150 muM. Under the same experimental condition, YLF-466D effectively inhibited aggregation induced by platelet agonists including thrombin, ADP and collagen. Such AMPK activation and aggregation inhibition were abolished by pretreatment with the AMPK inhibitors compound C (CC) and ara-A, indicating that antiaggregatory effect of YLF-466D is mediated by AMPK. YLF-466D induced an activation-dependent eNOS phosphorylation at Ser1177, an elevation of cyclic nucleotides cGMP and cAMP, and subsequent phosphorylation of vasodilator-stimulated phosphoprotein (VASP) at Ser239 and Ser157. All these events were prevented by CC and ara-A. In addition to isolated platelets, YLF-466D attenuated whole blood aggregation induced by collagen. Taken together, YLF-466D is capable of inhibiting platelet aggregation by activating AMPK and its downstream eNOS-cGMP-PKG signaling axis. This study reconfirms the antiplatelet activity of AMPK activators and suggests the potential application of YLF-466D to antiplatelet therapy, although the in vivo and clinical validation remains to be assessed.

Description

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

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