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CAY10499 Sale

(Synonyms: CAY10499) 目录号 : GC14244

A non-selective lipase inhibitor

CAY10499 Chemical Structure

Cas No.:359714-55-9

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1mg
¥158.00
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5mg
¥670.00
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10mg
¥1,170.00
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25mg
¥2,340.00
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产品描述

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].

References:
[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.

Chemical Properties

Cas No. 359714-55-9 SDF
别名 CAY10499
化学名 [4-(5-methoxy-2-oxo-1,3,4-oxadiazol-3(2H)-yl)-2-methylphenyl]-carbamic acid, phenylmethyl ester
Canonical SMILES CC1=CC(N(N=C(O2)OC)C2=O)=CC=C1NC(OCC3=CC=CC=C3)=O
分子式 C18H17N3O5 分子量 355.3
溶解度 20mg/mL in DMSO, 20mg/mL in DMF, 2mg/mL in Ethanol 储存条件 Store at -20°C, protect from light
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.8145 mL 14.0726 mL 28.1452 mL
5 mM 0.5629 mL 2.8145 mL 5.629 mL
10 mM 0.2815 mL 1.4073 mL 2.8145 mL
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