Date published: 2026-5-31

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LY2183240 (CAS 874902-19-9)

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Alternate Names:
5-Biphenyl-4-ylmethyl-tetrazole-1-carboxylic acid dimethylamide
Application:
LY2183240 is is a potent inhibitor of FAAH activity, and the uptake and enzymatic hydrolysis of anandamide
CAS Number:
874902-19-9
Purity:
≥98%
Molecular Weight:
307.35
Molecular Formula:
C17H17N5O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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LY2183240 is a potent inhibitor of the uptake (IC50= 7.3 nM) and enzymatic hydrolysis of anandamide (sc-205592). The compound also inhibits the activity of FAAH (fatty acid amide hydrolase)(IC50=12.4 nM) and other brain serine proteases. LY2183240 inhibits more effectively than the inhibitor of anandamide transport, N-(4-Hydroxyphenyl)-arachidonylamide (AM-404) (sc-200363). The endocannabinoid system, which anandamide is a part of, might play an important role in the central and peripheral regulation of pain.


LY2183240 (CAS 874902-19-9) References

  1. Identification of a high-affinity binding site involved in the transport of endocannabinoids.  |  Moore, SA., et al. 2005. Proc Natl Acad Sci U S A. 102: 17852-7. PMID: 16314570
  2. Modulation of neuropathic and inflammatory pain by the endocannabinoid transport inhibitor AM404 [N-(4-hydroxyphenyl)-eicosa-5,8,11,14-tetraenamide].  |  La Rana, G., et al. 2006. J Pharmacol Exp Ther. 317: 1365-71. PMID: 16510698
  3. Pharmacological characterization of endocannabinoid transport and fatty acid amide hydrolase inhibitors.  |  Dickason-Chesterfield, AK., et al. 2006. Cell Mol Neurobiol. 26: 407-23. PMID: 16736384
  4. The putative endocannabinoid transport blocker LY2183240 is a potent inhibitor of FAAH and several other brain serine hydrolases.  |  Alexander, JP. and Cravatt, BF. 2006. J Am Chem Soc. 128: 9699-704. PMID: 16866524
  5. Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: a critical revisitation.  |  Ortar, G., et al. 2008. Eur J Med Chem. 43: 62-72. PMID: 17452063
  6. Aqueous humor outflow effects of 2-arachidonylglycerol.  |  Njie, YF., et al. 2008. Exp Eye Res. 87: 106-14. PMID: 18597752
  7. Antinociceptive effects of tetrazole inhibitors of endocannabinoid inactivation: cannabinoid and non-cannabinoid receptor-mediated mechanisms.  |  Maione, S., et al. 2008. Br J Pharmacol. 155: 775-82. PMID: 18660824
  8. Effects of the novel endocannabinoid uptake inhibitor, LY2183240, on fear-potentiated startle and alcohol-seeking behaviors in mice selectively bred for high alcohol preference.  |  Powers, MS., et al. 2010. Psychopharmacology (Berl). 212: 571-83. PMID: 20838777
  9. Anticonvulsive effects of endocannabinoids; an investigation to determine the role of regulatory components of endocannabinoid metabolism in the Pentylenetetrazol induced tonic- clonic seizures.  |  Zareie, P., et al. 2018. Metab Brain Dis. 33: 939-948. PMID: 29504066
  10. LY2183240 regioisomers act as competitive and selective inhibitors of class C β-lactamases.  |  de Resende, PE., et al. 2023. Int J Antimicrob Agents. 61: 106774. PMID: 36893812

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

LY2183240, 10 mg

sc-200357
10 mg
$85.00

LY2183240, 50 mg

sc-200357A
50 mg
$333.00