874902-19-9
Chemical Structure
LY2183240
- CAS No.: 874902-19-9
- Formula:C17H17N5O
- Molecular Weight:307.35
IUPAC Name: 5-([1,1'-biphenyl]-4-ylmethyl)-N,N-dimethyl-1H-tetrazole-1-carboxamide
InChIKey: GZNIYOXWFCDBBJ-UHFFFAOYSA-N
SMILES: O=C(N(C)C)N1N=NN=C1CC(C=C2)=CC=C2C3=CC=CC=C3
Biological Activity: 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[1][2] [3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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LY2183240 | 98.00% | 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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LY2183240 (Standard) | ≥98% | 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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- [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]
Keywords
