A muscarinic M4 receptor positive allosteric modulator
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VU0152100

Item No. 32968

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-amino-N-[(4-methoxyphenyl)methyl]-4,6-dimethyl-thieno[2,3-b]pyridine-2-carboxamide
CAS Number
409351-28-6
Molecular Formula
C18H19N3O2S
Formula Weight
341.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml
λmax
218, 283 nm
SMILES
O=C(C1=C(N)C2=C(C)C=C(C)N=C2S1)NCC3=CC=C(C=C3)OC
InChi Code
InChI=1S/C18H19N3O2S/c1-10-8-11(2)21-18-14(10)15(19)16(24-18)17(22)20-9-12-4-6-13(23-3)7-5-12/h4-8H,9,19H2,1-3H3,(H,20,22)
InChi Key
MDNWGCQSCGNTKH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $104

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    10 mg

    $174

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    25 mg

    $409

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    Product Description

    VU0152100 is a positive allosteric modulator of M4 muscarinic acetylcholine receptors.1 It potentiates calcium mobilization induced by acetylcholine (ACh) in CHO-K1 cells expressing the rat M4 receptor with an EC50 value of 380 nM. VU0152100 is selective for M4 over M1, M2, M3 and M5 receptors, as well as a panel of 68 additional GPCRs, ion channels, transporters, and enzymes, but does bind to the benzodiazepine binding site of the GABAA receptor at 10 µM. It reduces cocaine-induced increases in locomotor activity and cocaine self-administration in mice when administered at a dose of 1 mg/kg.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Brady, A.E., Jones, C.K., Bridges, T.M., et al. Centrally active allosteric potentiators of the M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats. J. Pharmacol. Exp. Ther. 327(3), 941-953 (2008).

    2. Dencker, D., Weikop, P., Sørensen, G., et al. An allosteric enhancer of M4 muscarinic acetylcholine receptor function inhibits behavioral and neurochemical effects of cocaine. Psychopharmacology 224(2), 277-287 (2012).