A potent agonist of GPR139
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JNJ-63533054

Item No. 23450

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-chloro-N-[2-oxo-2-[[(1S)-1-phenylethyl]amino]ethyl]-benzamide
CAS Number
1802326-66-4
Molecular Formula
C17H17ClN2O2
Formula Weight
316.8
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 5 mg/ml
SMILES
ClC1=CC=CC(C(NCC(N[C@@H](C)C2=CC=CC=C2)=O)=O)=C1
InChi Code
InChI=1S/C17H17ClN2O2/c1-12(13-6-3-2-4-7-13)20-16(21)11-19-17(22)14-8-5-9-15(18)10-14/h2-10,12H,11H2,1H3,(H,19,22)(H,20,21)/t12-/m0/s1
InChi Key
MWDVCHRYCKXEBY-LBPRGKRZSA-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

    $103

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    10 mg

    $186

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    Product Description

    JNJ-63533054 is a potent agonist of the orphan G protein-coupled receptor GPR139 (EC50 = 16 nM in HEK293 cells expressing human GPR139).1 It is selective for GPR139 over 50 known G protein-coupled receptors, ion channels, and transporters as determined by an external selectivity panel. Tritium-labeled JNJ-63533054 has been used in displacement assays to identify physiological ligands of GPR139.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Dvorak, C.A., Coate, H., Nepomuceno, D., et al. Identification and SAR of glycine benzamides as potent agonists for the GPR139 receptor. ACS Med. Chem. Lett. 6(9), 1015-1018 (2015).

    2. Liu, C., Bonaventure, P., Lee, G., et al. GPR139, an orphan receptor highly enriched in the habenula and septum, is activated by the essential amino acids L-Tryptophan and L-Phenylalanine. Mol. Pharmacol. 88(5), 911-925 (2015).