A potent, competitive inhibitor of anandamide uptake
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LY2183240

Item No. 10008663

Product Insert (PDF)GC-MS (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-([1,1'-biphenyl]-4-ylmethyl)-N,N-dimethyl-1H-tetrazole-1-carboxamide
CAS Number
874902-19-9
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
253 nm
SMILES
O=C(N(C)C)N1N=NN=C1CC2=CC=C(C3=CC=CC=C3)C=C2
InChi Code
InChI=1S/C17H17N5O/c1-21(2)17(23)22-16(18-19-20-22)12-13-8-10-15(11-9-13)14-6-4-3-5-7-14/h3-11H,12H2,1-2H3
InChi Key
GZNIYOXWFCDBBJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $103

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    5 mg

    $278

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    Product Description

    LY2183240 is a potent, competitive inhibitor of anandamide uptake (IC50 = 270 pM; Ki = 540 pM) and hydrolysis.1,2,3 It increases 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

    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).