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    LY2119620
    LY2119620

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1165
    CAS #: 886047-22-9Purity ≥98%

    Description: LY2119620 (LY 2119620; LY-2119620) is a novel, potent, specific, high-affinity and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors, the so called positive allosteric modulator (PAM). LY2033298 enhances inhibition by oxotremorine of light-induced phase shifts in hamster circadian activity rhythms. In [35S]GTPγS-binding experiments, LY2119620 exhibited a modest allosteric agonism of 23.2% and 16.8% at the M2 and M4 receptors, respectively. LY2119620 and ACh binding caused cooperativity factor α of 79.4 and 19.5 for the M4 receptor and the M2 receptor, respectively. 

    References: Mol Pharmacol. 2014 Jul;86(1):106-15; Mol Pharmacol. 2014 Jul;86(1):116-23.

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    Molecular Weight (MW)437.94
    FormulaC19H24ClN5O3S
    CAS No.886047-22-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 87 mg/mL (198.7 mM)
    Water: <1 mg/mL
    Ethanol: 10 mg/mL(22.8 mM)
    Other infoChemical Name: 3-amino-5-chloro-N-cyclopropyl-4-methyl-6-[2-(4-methyl-1-piperazinyl)-2-oxoethoxy]-thieno[2,3-b]pyridine-2-carboxamide
    InChi Key: TYTGOXSAAQWLPJ-UHFFFAOYSA-N
    InChi Code: InChI=1S/C19H24ClN5O3S/c1-10-13-15(21)16(17(27)22-11-3-4-11)29-19(13)23-18(14(10)20)28-9-12(26)25-7-5-24(2)6-8-25/h11H,3-9,21H2,1-2H3,(H,22,27)
    SMILES Code: O=C(C1=C(N)C2=C(C)C(Cl)=C(OCC(N3CCN(C)CC3)=O)N=C2S1)NC4CC4
    SynonymsLY2119620; LY 2119620; LY-2119620


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    In Vitro

    In vitro activity: LY2119620 displays modest allosteric agonism and positively modulates the functional G protein–signaling ability of an agonist at the M2/M4 receptor subtypes by placing the M2 and M4 receptors into an active G protein–bound state. LY2119620 enhances the potency of three muscarinic acetylcholine receptor agonists, ACh, Oxo-M and iperoxo. [3H]LY2119620 can be used as a probe for the human M(2) and M(4) muscarinic receptor allosteric binding sites.


    Kinase Assay: [3H]LY2119620 equilibrium binding is achieved by incubating 15 µg membranes, orthosteric ligand (100 µM), and various concentrations of [3H]LY2119620 (0.2 to 60 nM) for 1 hour at 25°C. The specific binding versus time data are fit to a one-site specific binding model, and the Bmax and Kd for the allosteric molecule are calculated for each orthosteric ligand.  


    Cell Assay: In [35S]GTPγS-binding experiments, LY2119620 exhibited a modest allosteric agonism of 23.2% and 16.8% at the M2 and M4 receptors, respectively. LY2119620 and ACh binding caused cooperativity factor α of 79.4 and 19.5 for the M4 receptor and the M2 receptor, respectively. The cooperativity between LY2119620 and orthosteric agonists (Iperoxo or Oxo-M) was also observed. M2 receptor simultaneously bound to LY2119620 and iperoxo. LY2119620 exhibited mild negative cooperativity with the inverse agonist NMS and strong positive cooperativity with iperoxo. LY2119620 significantly increased Bmax values without changes in Kd when cooperativity binding of [3H]LY2119620 with mAChR, suggesting a G protein-dependent process.

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    ReferencesMol Pharmacol. 2014 Jul;86(1):106-15; Mol Pharmacol. 2014 Jul;86(1):116-23.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    LY2119620

    Functional agonism of the M2 and M4 receptors measured using [35S]GTPγS-binding. Mol Pharmacol. 2014 Jul;86(1):106-15.
     

    LY2119620

    [35S]GTPγS-binding at the M2 and M4 receptors in the presence of LY2119620. Mol Pharmacol. 2014 Jul;86(1):106-15.
     

    LY2119620

    Orthosteric and allosteric radioligand saturation-binding studies at the M2 and M4 receptors. Mol Pharmacol. 2014 Jul;86(1):106-15.


    LY2119620

    [3H]NMS kinetic and equilibrium studies in the presence of LY2119620.


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