LY2183240 (Standard)
LY2183240 (Standard) is the analytical standard of LY2183240 (HY-10865). This product is intended for research and analytical applications. LY2183240 is a highly potent blocker of anandamide uptake (IC50= 270 pM; Ki=540 nM). LY2183240 is a potent, covalent inhibitor of the endocannabinoid-degrading enzyme fatty acid amide hydrolase (FAAH) with an IC50 of 12.4 nM. LY2183240 inactivates FAAH by carbamylation of the enzyme's serine nucleophile. LY2183240 also inhibits several other brain serine hydrolases with IC50s of 5.3, 0.09, 8.2 nM for MAG lipase, bh6 and KiAA1363, respectively .
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 874902-19-9
- 分子式: C17H17N5O
- 分子量:307.35
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Product Information
The compound is the grade of analytical standard, which is the reference standard supplied assay. It is commonly used in qualitative, quantitative and methodological research experiments in HPLC, GC and MS.
化学情報
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CAS 番号 874902-19-9
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分子量 307.35
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分子式 C17H17N5O
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SMILES
O=C(N(C)C)N1N=NN=C1CC(C=C2)=CC=C2C3=CC=CC=C3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Moore SA, et al. Identification of a high-affinity binding site involved in the transport of endocannabinoids. Proc Natl Acad Sci U S A. 2005;102(49):17852-17857. [Content Brief]
[2]. Sun L, et al. Endocannabinoid activation of CB1 receptors contributes to long-lasting reversal of neuropathic pain by repetitive spinal cord stimulation. Eur J Pain. 2017 May;21(5):804-814. [Content Brief]
[3]. Alexander JP, Cravatt BF. The putative endocannabinoid transport blocker LY2183240 is a potent inhibitor of FAAH and several other brain serine hydrolases. J Am Chem Soc. 2006 Aug 2;128(30):9699-704. [Content Brief]
[4]. Maione S, et al. Antinociceptive effects of tetrazole inhibitors of endocannabinoid inactivation: cannabinoid and non-cannabinoid receptor-mediated mechanisms. Br J Pharmacol. 2008 Nov;155(5):775-82. [Content Brief]
[5]. Pelorosso FG, et al. The endocannabinoid anandamide inhibits kinin B1 receptor sensitization through cannabinoid CB1 receptor stimulation in human umbilical vein. Eur J Pharmacol. 2009 Jan 5;602(1):176-9. [Content Brief]
[6]. Powers MS, et al. Effects of the novel endocannabinoid uptake inhibitor, LY2183240, on fear-potentiated startle and alcohol-seeking behaviors in mice selectively bred for high alcohol preference. Psychopharmacology (Berl). 2010 Dec;212(4):571-83. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)