CAY10499

A non-selective lipase inhibitor

此产品仅用于科学研究，我们不为任何个人用途提供产品和服务

库存: 现货

可选规格

包装

价格

促销价

数量
1mg

￥175.00

140.00

- +
5mg

￥812.00

650.00

- +
10mg

￥1412.00

1130.00

- +
25mg

￥2825.00

2260.00

- +

已选 0 种 0 瓶

金额: ￥0.00

首页收藏

货号: ajci12730
CAS: 359714-55-9
别名: CAY10499
分子式: C18H17N3O5
分子量: 355.3
纯度: >98%
溶解度: 20mg/mL in DMSO, 20mg/mL in DMF, 2mg/mL in Ethanol
储存: Store at -20°C, protect from light
库存: 现货

Background

CAY10499 is a potent inhibitor of monoglyceride lipase (MGL) [1] and human hormone sensitive lipase [2].

Monoglyceride lipase (MGL) plays an important role in the metabolism of the lipid transmitter 2-arachidonoylglycerol (2-AG). This endocannabinoid has been known to mediate various physiological processes, and its regulation is thought to be of great therapeutic potential[1]. Hormone sensitive lipase (HSL) has been involved in catalyzing the hydrolysis of tri-, di-, and monoacylglycerols, and cholesterol esters, thus mobilizing fatty acids as a primary source of energy in mammals. The HSL enzyme is highly expressed in adipose tissue and steroidogenic tissue and implicated in diverse physiology roles including those in steroidogenesis and spermatogenesis, foam cell formation in atherosclerosis, and diabetes [3].

CAY10499 inhibited MGL-mediated 4-NPA hydrolysis with the IC 50 value of 0.5 ± 0.03 μM. CAY10499 fully inhibited [3H]-AEA hydrolysis by human recombinant FAAH with an IC50 of 76 nM. CAY10499 displaced only 25% and 20% of [3H]-CP-55940-specific binding to the CB1 and CB2 receptors, respectively [1]. CAY10499 potently inhibited the activity of human hormone sensitive lipase with an IC50 of 90 nM for the recombinant human hormone sensitive lipase enzyme [2].

参考文献:
[1] Muccioli G G, Labar G, Lambert D M.? CAY10499, a novel monoglyceride lipase inhibitor evidenced by an expeditious MGL assay[J]. ChemBioChem, 2008, 9(16): 2704-2710.
[2] Ben Ali Y, Muller G, Petry S, et al.? Kinetic characterization and specific inhibition of hormone sensitive lipase[C]//CHEMISTRY AND PHYSICS OF LIPIDS. ELSEVIER HOUSE, BROOKVALE PLAZA, EAST PARK SHANNON, CO, CLARE, 00000, IRELAND: ELSEVIER IRELAND LTD, 2005, 136(2): 155-155.
[3] Kraemer F B, Shen W J.? Hormone-sensitive lipase control of intracellular tri-(di-) acylglycerol and cholesteryl ester hydrolysis[J]. Journal of lipid research, 2002, 43(10): 1585-1594.