A brain penetrant positive allosteric modulator of the mGluR5
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LSN2463359

Item No. 22104

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(1-methylethyl)-5-[2-(4-pyridinyl)ethynyl]-2-pyridinecarboxamide
CAS Number
1401031-52-4
Molecular Formula
C16H15N3O
Formula Weight
265.3
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/ml
λmax
215, 247, 297 nm
SMILES
O=C(NC(C)C)C(C=C1)=NC=C1C#CC2=CC=NC=C2
InChi Code
InChI=1S/C16H15N3O/c1-12(2)19-16(20)15-6-5-14(11-18-15)4-3-13-7-9-17-10-8-13/h5-12H,1-2H3,(H,19,20)
InChi Key
STAFRSGTRKNXHF-UHFFFAOYSA-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

    $110

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    10 mg

    $203

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    25 mg

    $454

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    Product Description

    LSN2463359 is a positive allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5; EC50 = 24 nM).1 It is without effect at other mGluRs. LSN2463359 is brain penetrant and reverses learning deficits in a rat model of schizophrenia.1,2 Through its effects on mGluR5, LSN2463359 attenuates deficits in performance in operant behavior induced by SDZ-220581, an NMDA (Item No. 14581) receptor antagonist, in rats.3,2 It also promotes wakefulness in animals.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gastambide, F., Cotel, M.-C., Gilmour, G., et al. Selective remediation of reversal learning deficits in the neurodevelopmental MAM model of schizophrenia by a novel mGlu5 positive allosteric modulator. Neuropsychopharmacology 37(4), 1057-1066 (2012).

    2. Gilmour, G., Broad, L.M., Wafford, K.A., et al. In vitro characterisation of the novel positive allosteric modulators of the mGlu5 receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the rat. Neuropharmacology 64, 224-239 (2013).

    3. Gastambide, F., Gilmour, G., Robbins, T.W., et al. The mGlu₅ positive allosteric modulator LSN2463359 differentially modulates motor, instrumental and cognitive effects of NMDA receptor antagonists in the rat. Neuropharmacology 64, 240-247 (2013).