An agonist of mGluR2 and mGluR3
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LY404039

Item No. 18408

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(1R,4S,5S,6S)-4-amino-2-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid 2,2-dioxide
CAS Number
635318-11-5
Molecular Formula
C7H9NO6S
Formula Weight
235.2
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
PBS (pH 7.2): 0.5 mg/mL
SMILES
O=S1([C@]([C@@H]2C(O)=O)([H])[C@]2([H])[C@@](C(O)=O)(N)C1)=O
InChi Code
InChI=1S/C7H9NO6S/c8-7(6(11)12)1-15(13,14)4-2(3(4)7)5(9)10/h2-4H,1,8H2,(H,9,10)(H,11,12)/t2-,3-,4+,7+/m1/s1
InChi Key
AVDUGNCTZRCAHH-MDASVERJSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $90

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    10 mg

    $159

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    25 mg

    $354

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    Product Description

    LY404039 is a potent agonist of metabotropic glutamate (mGlu) group II receptors mGluR2 and mGluR3 (Kis = 149 and 62 nM, respectively, for recombinant human isoforms).1 It displays 100-fold selectivity for mGluR2/3 over ionotropic glutamate receptors, glutamate transporters, and several other receptors targeted by known anxiolytic and antipsychotic medications.1 LY404039 inhibits the binding of domperidone (Item No. 18875) by 15.5% to dopamine D2 receptors (Kd = ~10 nM in vitro), indicating interaction with this receptor.2 LY404039 is orally bioavailable and demonstrates antipsychotic and anxiolytic efficacy in several animal models.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Rorick-Kehn, L.M., Johnson, B.G., Burkey, J.L., et al. Pharmacological and pharmacokinetic properties of a structurally novel, potent, and selective metabotropic glutamate 2/3 receptor agonist: in vitro characterization of agonist (−)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]-hexane-4,6-dicarboxylic acid (LY404039). J. Pharmacol. Exp. Ther. 321(1), 308-317 (2007).

    2. Seeman, P., and Guan, H.C. Glutamate agonist LY404,039 for treating schizophrenia has affinity for the dopamine D2(High) receptor. Synapse 63(10), 935-939 (2009).

    3. Rorick-Kehn, L.M., Johnson, B.G., Knitowski, K.M., et al. In vivo pharmacological characterization of the structurally novel, potent, selective mGlu2/3 receptor agonist LY404039 in animal models of psychiatric disorders. Psychopharmacology (Berl) 193(1), 121-136 (2007).