CAY10499
(Synonyms: CAY10499) 目录号 : GC14244A non-selective lipase inhibitor
Cas No.:359714-55-9
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
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 |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 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。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
||
Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
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 |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。