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Merck

A1737

A922500

synthetic (organic), >95% (HPLC), Diacylglycerol acyltransferase inhibitor, powder

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この商品について

実験式(ヒル表記法):
C26H24N2O4
CAS番号:
分子量:
428.48
MDL number:
UNSPSC Code:
12352204
NACRES:
NA.77
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製品名

A922500,

SMILES string

N(c2ccc(cc2)c3ccc(cc3)C(=O)[C@H]4[C@@H](CCC4)C(=O)O)C(=O)Nc1ccccc1

InChI

1S/C26H24N2O4/c29-24(22-7-4-8-23(22)25(30)31)19-11-9-17(10-12-19)18-13-15-21(16-14-18)28-26(32)27-20-5-2-1-3-6-20/h1-3,5-6,9-16,22-23H,4,7-8H2,(H,30,31)(H2,27,28,32)/t22-,23-/m1/s1

InChI key

BOZRFEQDOFSZBV-DHIUTWEWSA-N

biological source

synthetic (organic)

assay

>95% (HPLC)

form

powder

mol wt

Mw 428.5

solubility

DMSO: 10 mg/mL, clear, colorless to greenish-yellow

storage temp.

−20°C

Quality Level

Application

A922500 has been used in the inhibition of diacylglycerol acyltransferase (DGAT) in epithelial human breast cancer cell line (MDA-MB-231), digitonin-permeabilized human cancer cells, human myotubes and macrophages.

Biochem/physiol Actions

Diacylglycerol acyltransferase (DGAT-1) inhibitor; IC50 7 to 24 nM
The diacylglycerol acyltransferase (DGAT) 1 inhibitor A922500 was shown to effectively reduce postprandial serum triglyceride levels in rodents at concentrations of 0.03, 0.3 and 3 mg/kg. These results suggest A922500 may have beneficial effects in reducing the risk of cardiovascular disease.

Physical form

A922500 is supplied as a crystalline solid.

Preparation Note

A stock solution may be made by dissolving the A922500 in the solvent of choice. A922500 is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF).

保管分類

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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文書ライブラリにアクセスする

A Snake Venom-Secreted Phospholipase A2 Induces Foam Cell Formation Depending on the Activation of Factors Involved in Lipid Homeostasis
Leiguez E, et al.
Mediators of Inflammation, 2018 (2018)
Andrew J King et al.
European journal of pharmacology, 637(1-3), 155-161 (2010-04-14)
Postprandial serum triglyceride concentrations have recently been identified as a major, independent risk factor for future cardiovascular events. As a result, postprandial hyperlipidemia has emerged as a potential therapeutic target. The purpose of this study was two-fold. Firstly, to describe
Increased triacylglycerol-Fatty acid substrate cycling in human skeletal muscle cells exposed to eicosapentaenoic acid
Lovsletten NG, et al.
PLoS ONE, 13(11), e0208048-e0208048 (2018)
A specific lipid metabolic profile is associated with the epithelial mesenchymal transition program
Giudetti AM, et al.
Biochimica et Biophysica Acta - Molecular and Cell Biology of Lipids, 1864(3), 344-357 (2019)
Lipid droplets induced by secreted phospholipase A2 and unsaturated fatty acids protect breast cancer cells from nutrient and lipotoxic stress
Jarc E, et al.
Biochimica et Biophysica Acta - Molecular and Cell Biology of Lipids, 1863(3), 247-265 (2018)

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