JNJ-3792165 | GPR139 antagonist

CAS:
 353504-63-9
Catalog Number:
 10-5863

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JNJ-3792165 (353504-63-9) is a potent and selective antagonist at GPR139, a non-canonical opioid receptor. It has high affinity for human GPR139 (pKi = 7.7, displacement of [3H] JNJ-6353054) and behaves as an antagonist in a [35S]GTPγS assay (pKb = 7.4) and calcium mobilization assay.1 It displayed no significant affinity in a selectivity screen of over 50 other neurotransmitter and neuropeptide receptors (less than 50% inhibition at 1 μM).1 Completely blocks (10 mM) the effects of optogenetic stimulation of dynorphin release in dynorphinergic neurons of the nucleus accumbens at 10 mM.2 JNJ-3792165 is an important new tool for exploring the biology of GPR139.3,4

References/Citations:

  1. Nepomuceno et al. (2018), Re-evaluation of Adrenocorticotropic Hormone and Melanocyte Stimulating Hormone Activation of GPR139 in Vitro; Front. Pharmacol., 9 157
  2. Li et al. (2025), Homeostatic scaling of dynorphin signaling by a non-canonical opioid receptor; Nat. Commun., 16 6786
  3. Vedel et al. (2020), Pharmacology and function of the orphan GPR139 G protein‐coupled receptor; Basic Clin. Pharmacol. Toxicol., 126 (Suppl 6) 35
  4. Pallareti et al. (2023), Pharmacological characterization of novel small molecule agonists and antagonists for the orphan receptor GPR139; Eur. J. Pharmacol., 943 175553
353504-63-9, GPR139, GPR139 antagonist, JNJ-3792165, JNJ-3792165 supplier, JNJ3792165
CAS:
353504-63-9
Catalog Number:
10-5863
Activity:
GPR139 antagonist
Chemical Names:
1-(2,6-Dichlorobenzyl)-5-methyl-N-(m-tolyl)-1H-pyrazole-3-carboxamide
Molecular Weight:
374.27
Molecular Formula:

C19H17Cl2N3O

Solubility:
Soluble in DMSO (70 mg/ml)
Physical Properties:
White solid
Purity:

98% TLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ room temperature. Solutions in DMSO may be stored at -20°C for up to 2 months.
Shipping Code:
RT

Safety Data Sheet:

Download Safety Data Sheet

Product Data Sheet:

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JNJ-3792165 (353504-63-9) is a potent and selective antagonist at GPR139, a non-canonical opioid receptor. It has high affinity for human GPR139 (pKi = 7.7, displacement of [3H] JNJ-6353054) and behaves as an antagonist in a [35S]GTPγS assay (pKb = 7.4) and calcium mobilization assay.1 It displayed no significant affinity in a selectivity screen of over 50 other neurotransmitter and neuropeptide receptors (less than 50% inhibition at 1 μM).1 Completely blocks (10 mM) the effects of optogenetic stimulation of dynorphin release in dynorphinergic neurons of the nucleus accumbens at 10 mM.2 JNJ-3792165 is an important new tool for exploring the biology of GPR139.3,4

References/Citations:

  1. Nepomuceno et al. (2018), Re-evaluation of Adrenocorticotropic Hormone and Melanocyte Stimulating Hormone Activation of GPR139 in Vitro; Front. Pharmacol., 9 157
  2. Li et al. (2025), Homeostatic scaling of dynorphin signaling by a non-canonical opioid receptor; Nat. Commun., 16 6786
  3. Vedel et al. (2020), Pharmacology and function of the orphan GPR139 G protein‐coupled receptor; Basic Clin. Pharmacol. Toxicol., 126 (Suppl 6) 35
  4. Pallareti et al. (2023), Pharmacological characterization of novel small molecule agonists and antagonists for the orphan receptor GPR139; Eur. J. Pharmacol., 943 175553

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