A GPR139 antagonist
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LP-471756

Item No. 46415

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-cyclohexyl-N-(2-methylphenyl)-benzenesulfonamide
CAS Number
413605-11-5
Molecular Formula
C19H23NO2S
Formula Weight
329.5
Purity
≥98%
Formulation (Request formulation change)
A solid
SMILES
CC1=C(C=CC=C1)NS(C(C=C2)=CC=C2C3CCCCC3)(=O)=O
InChi Code
InChI=1S/C19H23NO2S/c1-15-7-5-6-10-19(15)20-23(21,22)18-13-11-17(12-14-18)16-8-3-2-4-9-16/h5-7,10-14,16,20H,2-4,8-9H2,1H3
InChi Key
STLMNZVBCJVQOZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $25

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    5 mg

    $75

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    10 mg

    $125

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    Product Description

    LP-471756 is an antagonist of G protein-coupled receptor 139 (GPR139), which is expressed in the brain in humans.1 It inhibits GPR139 agonist-induced cAMP production in GPR139-expressing HEK293F cells (IC50 = 640 nM). LP-471756 inhibits calcium signaling in GPR139-expressing CHO cells (IC50 = 2,933 nM) but also fully inhibits calcium mobilization in M1 muscarinic acetylcholine receptor-expressing CHO cells at 100 µM.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hu, L.A., Tang, P.M., Eslahi, N.K., et al. Identification of surrogate agonists and antagonists for orphan G-protein-coupled receptor GPR139. J. Biomol. Screen. 14(7), 789-797 (2009).

    2. Pallareti, L., Rath, T.F., Trapkov, B., et al. Pharmacological characterization of novel small molecule agonists and antagonists for the orphan receptor GPR139. Eur. J. Pharmacol. 943, 175553 (2023).