LY 2183240

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Cat.No. 2452 - LY 2183240 | C17H17N5O | CAS No. 874902-19-9
Description: Novel, potent anandamide uptake inhibitor; inhibits FAAH
Chemical Name: 5-[(1,1'-Biphenyl]-4-yl)methyl]-N,N-dimethyl-1H-tetrazole-1-carboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews
Literature

Biological Activity

Novel and highly potent blocker of anandamide uptake (IC50 = 270 pM). Inhibits fatty acid amide hydrolase (FAAH) activity (IC50 = 12.4 nM). Following i.p. administration in rats, increases brain anandamide concentration and exerts antinociceptive effects in formalin model of pain.

Licensing Information

Sold under license from Eli Lilly and Company

Compound Libraries

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Technical Data

M. Wt 307.35
Formula C17H17N5O
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 874902-19-9
PubChem ID 11507802
InChI Key GZNIYOXWFCDBBJ-UHFFFAOYSA-N
Smiles CN(C)C(=O)N1N=NN=C1CC1=CC=C(C=C1)C1=CC=CC=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 30.74 100
ethanol 15.37 50 with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 307.35. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.25 mL 16.27 mL 32.54 mL
5 mM 0.65 mL 3.25 mL 6.51 mL
10 mM 0.33 mL 1.63 mL 3.25 mL
50 mM 0.07 mL 0.33 mL 0.65 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

Dickason-Chesterfield et al (2006) Pharmacological characterization of endocannabinoid transport and fatty acid amide hydrolase inhibitors. Cell Mol.Neurobiol. 26 407 PMID: 16736384

Alexander and Cravat (2006) The putative endocannabinoid transport blocker LY2183240 is a potent inhibitor of FAAH and several other brain serine hydrolases. J.Am.Chem.Soc. 128 9699 PMID: 16866524

Moore et al (2005) Identification of a high-affinity binding site involved in the transport of endocannabinoids. Proc.Natl.Acad.Sci.USA 102 17852


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Keywords: LY 2183240, LY 2183240 supplier, FAAH, inhibitors, inhibits, anandamide, reuptake, potent, Anandamide, Amidase, Fatty, Acid, Amide, Hydrolases, AMT, Transporters, cannabinoids, Monoamine, Neurotransmitter, LY2183240, Cannabinoid, Hydrolase, (FAAH), Other, Cannabinoids, 2452, Tocris Bioscience

1 Citation for LY 2183240

Citations are publications that use Tocris products. Selected citations for LY 2183240 include:

Gonzalez-Islas et al (2012) Tonic and transient endocannabinoid regulation of AMPAergic miniature postsynaptic currents and homeostatic plasticity in embryonic motor networks. PLoS One 32 13597 PMID: 23015449


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Literature in this Area

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Cannabinoid Receptor Ligands Scientific Review

Written by Roger Pertwee, this review discusses compounds which affect the activity of the endocannabinoid system, focusing particularly on ligands that are most widely used as experimental tools and denotes compounds available from Tocris.