A less potent, 2,5-regioisomer of LY2183240
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LY2183240 2’-isomer

Item No. 14523

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-([1,1'-biphenyl]-4-ylmethyl)-N,N-dimethyl-2H-tetrazole-2-carboxamide
CAS Number
1010096-65-7
Molecular Formula
C17H17N5O
Formula Weight
307.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMSO: 2 mg/mlEthanol: 10 mg/mlEthanol:PBS(pH 7.2) (1:5): 0.1 mg/ml
λmax
251 nm
SMILES
O=C(N(C)C)N1N=NC(CC(C=C2)=CC=C2C3=CC=CC=C3)=N1
InChi Code
InChI=1S/C17H17N5O/c1-21(2)17(23)22-19-16(18-20-22)12-13-8-10-15(11-9-13)14-6-4-3-5-7-14/h3-11H,12H2,1-2H3
InChi Key
VBVLSXPOMAONNK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    LY2183240 (Item No. 10008663) is a potent, competitive small molecule inhibitor of anandamide uptake (IC50 = 270 pM; Ki = 540 pM) and hydrolysis.1,2,3 It has been shown to increase anandamide levels in rat cerebellum (ED50 = 1.37 mg/kg) and displays dose-dependent efficacy (3-30 mg/kg) in several rodent models of persistent pain.1 LY2183240 2’-isomer is a less potent, 2,5-regioisomer of LY2183240 that inhibits anandamide hydrolysis and uptake with IC50 values of 33 and 998 nM, respectively.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Moore, S.A., Nomikos, G.G., Dickason-Chesterfield, A.K., et al. Identification of a high-affinity binding site involved in the transport of endocannabinoids. Proc. Natl. Acad. Sci. USA 102(49), 17852-17857 (2005).

    2. Ortar, G., Cascio, M.G., Moriello, A.S., et al. Carbamoyl tetrazoles as inhibitors of endocannabinoid inactivation: A critical revisitation. Eur. J. Med. Chem. 43(1), 62-72 (2008).

    3. Di Marzo, V. Targeting the endocannabinoid system: To enhance or reduce? Nat. Rev. Drug Discov. 7(5), 438-455 (2008).