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JZL195

强效双重FAAH / MAGL抑制剂

规格或纯度: 98%

CAS编号: 1210004-12-8
分子式: C₂₄H₂₃N₃O₅
分子量: 433.5
PubChem编号: 46232606

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货号 (SKU)	包装规格	是否现货	价格	数量
J276066-5mg	5mg	现货
J276066-10mg	10mg	现货
J276066-25mg	25mg	现货
J276066-50mg	50mg	现货
J276066-100mg	100mg	现货

查看相关系列

acyloxyacyl hydrolase Inhibitor Fatty acid amide hydrolase Inhibitor Monoacylglycerol lipase Inhibitor

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基本描述

规格或纯度	98%
英文名称	JZL195
别名	4-[(3-苯氧基苯基)甲基]-1-哌嗪羧酸4-硝基苯酯盐酸盐,
英文别名	JZL195\|1210004-12-8\|JZL 195\|JZL-195\|(4-nitrophenyl) 4-[(3-phenoxyphenyl)methyl]piperazine-1-carboxylate\|TP6P2HKJ54\|4-nitrophenyl 4-(3-phenoxybenzyl)piperazine-1-carboxylate\|CHEMBL606201\|4-Nitrophenyl 4-((3-phenoxyphenyl)methyl)-1-piperazinecarboxylate\|4-N
生化机理	JZL195 is a potent dual inhibitor of Monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH), enzymes that degrade the endocannabinoids 2-arachidonoylglycerol (2-AG) and anandamide (AEA), the endogenous ligands for the cannabinoid G-protein coupled receptors CB1 and CB2. IC50 values are 2 nM for MAGL and 4 nM for FAAH. JZL195 has been shown to inhibit endocannabinoid hydrolysis and elevate 2-AG and AEA levels in vivo.
储存温度	-20°C储存,干燥
运输条件	超低温冰袋运输
备注	如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
产品介绍	JZL195是有效的FAAH和MAGL抑制剂，IC50分别为2 nM和4 nM ?JZL195 has been used: as a selective inhibitor of endocannabinoid (eCB) clearance enzymes to induce in vivo long-term depression at CA3-CA1 synapses and at prelimbic (PrL)-nucleus accumbens (NAc)synapses, to study the neuroprotective action of eCB to inhibit the action of hydrolytic enzymes that limit eCB activity, to study the effect of 2-linoleoylglycerol (2-LG) on the human CB1 receptor activity as a dual fatty acid amide hydrolase (FAAH)/monoacylglycerol lipase (MAGL) inhibitor to study its dose-related antipruritic effect on the serotonin (5-HT)-induced scratching model

名称和标识符

IUPAC Name	(4-nitrophenyl) 4-[(3-phenoxyphenyl)methyl]piperazine-1-carboxylate
INCHI	InChI=1S/C24H23N3O5/c28-24(32-22-11-9-20(10-12-22)27(29)30)26-15-13-25(14-16-26)18-19-5-4-8-23(17-19)31-21-6-2-1-3-7-21/h1-12,17H,13-16,18H2
InChi Key	QNYRAEKLMNDRFY-UHFFFAOYSA-N
Canonical SMILES	C1CN(CCN1CC2=CC(=CC=C2)OC3=CC=CC=C3)C(=O)OC4=CC=C(C=C4)[N+](=O)[O-]
PubChem CID	46232606
分子量	433.5

数据库链接

PubChem CID	46232606
ChEMBL Ligand	CHEMBL606201
CAS Registry No.	1210004-12-8

化学和物理性质

溶解性	Soluble in DMSO to 100 mM

关联配体

Ligand ID	8606
名称	JZL195
别名	JZL-195
类别	Synthetic organic
学名	(4-nitrophenyl) 4-[(3-phenoxyphenyl)methyl]piperazine-1-carboxylate
生物活性评价	The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价	JZL195 was first reported as a dual inhibitor of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MGLL, a.k.a. MAGL) in 2009 . Animal experiments suggest that dual FAAH/MAGL inhibitiors may have improved analgesic effects against neuropathic pain, in comparison to selective FAAH and MAGL inhibitors, or cannabinoid receptor agonists . JZL195 has since been reported to also inhibit acyloxyacyl hydrolase (AOAH)

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参考文献

1. Long JZ, Nomura DK, Vann RE, Walentiny DM, Booker L, Jin X, Burston JJ, Sim-Selley LJ, Lichtman AH, Wiley JL et al.. (2009) Dual blockade of FAAH and MAGL identifies behavioral processes regulated by endocannabinoid crosstalk in vivo.. Proc Natl Acad Sci USA, 106 (48): (20270-5). [PMID:19918051]
2. Anderson WB, Gould MJ, Torres RD, Mitchell VA, Vaughan CW. (2014) Actions of the dual FAAH/MAGL inhibitor JZL195 in a murine inflammatory pain model.. Neuropharmacology, 81 (13): (224-30). [PMID:24384256]
3. Sakin YS, Dogrul A, Ilkaya F, Seyrek M, Ulas UH, Gulsen M, Bagci S. (2015) The effect of FAAH, MAGL, and Dual FAAH/MAGL inhibition on inflammatory and colorectal distension-induced visceral pain models in Rodents.. Neurogastroenterol Motil, 27 (7): (936-44). [PMID:25869205]
4. Ghosh S, Kinsey SG, Liu QS, Hruba L, McMahon LR, Grim TW, Merritt CR, Wise LE, Abdullah RA, Selley DE et al.. (2015) Full Fatty Acid Amide Hydrolase Inhibition Combined with Partial Monoacylglycerol Lipase Inhibition: Augmented and Sustained Antinociceptive Effects with Reduced Cannabimimetic Side Effects in Mice.. J Pharmacol Exp Ther, 354 (2): (111-20). [PMID:25998048]
5. Adamson Barnes NS, Mitchell VA, Kazantzis NP, Vaughan CW. (2016) Actions of the dual FAAH/MAGL inhibitor JZL195 in a murine neuropathic pain model.. Br J Pharmacol, 173 (1): (77-87). [PMID:26398331]
6. Bachovchin DA, Koblan LW, Wu W, Liu Y, Li Y, Zhao P, Woznica I, Shu Y, Lai JH, Poplawski SE et al.. (2014) A high-throughput, multiplexed assay for superfamily-wide profiling of enzyme activity.. Nat Chem Biol, 10 (8): (656-63). [PMID:24997602]

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