貨號	規格	價格	上海	北京	武漢	南京
S86976-10mg	98.8%	￥270.00 S86976-10mg ￥270.00 現貨	10 10	-	-	-
S86976-50mg	98.8%	￥910.00 S86976-50mg ￥910.00 現貨	2 2	-	-	-
S86976-100mg	≥98%	￥1430.00 S86976-100mg ￥1430.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

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

產品描述：

靶點：

FAAH;Autophagy

體內研究：

LY2183240 (3-30mg/kg; i.p.) dose-dependently attenuates formalin-induced paw-licking pain behavior in the formalin model of persistent pain mechanisms Animal Model: Male Sprague-Dawley rats (Formalin Pain Model) Dosage: 3, 10, 30 mg/kg Administration: I.p. Result: Dose-dependently attenuated formalin-induced paw-licking pain behavior in the formalin model of persistent pain mechanisms.

參考文獻：

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. 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. 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. 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. 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. 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

溶解性：

Soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	3.254 ml	16.268 ml	32.536 ml
5 mM	0.651 ml	3.254 ml	6.507 ml
10 mM	0.325 ml	1.627 ml	3.254 ml
50 mM	0.065 ml	0.325 ml	0.651 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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LY2183240

5-([1,1'-biphenyl]-4-ylmethyl)-N,N-dimethyl-1H-tetrazole-1-carboxamide