1. GPCR/G Protein
    Neuronal Signaling
  2. GPR139
  3. JNJ-63533054

JNJ-63533054 

Cat. No.: HY-19838 Purity: 99.94%
Handling Instructions

JNJ-63533054 is a potent and selective agonist of hGPR139 with an EC50 = 16 nM.

For research use only. We do not sell to patients.

JNJ-63533054 Chemical Structure

JNJ-63533054 Chemical Structure

CAS No. : 1802326-66-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 86 In-stock
Estimated Time of Arrival: December 31
5 mg USD 78 In-stock
Estimated Time of Arrival: December 31
10 mg USD 132 In-stock
Estimated Time of Arrival: December 31
50 mg USD 504 In-stock
Estimated Time of Arrival: December 31
100 mg USD 828 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

JNJ-63533054 is a potent and selective agonist of hGPR139 with an EC50 = 16 nM. IC50 value: 16 nM (EC50) Target: hGPR139 in vitro: JNJ-63533054 is a selective small-molecule agonist. JNJ-63533054 specifically activates human GPR139 in the calcium mobilization (EC50 = 16 ± 6 nM) and GTPγS binding (EC50 = 17 ± 4 nM) assays. [2] JNJ-63533054 is found to be clean of any cross reactivity as judged by an external selectivity panel of 50 known GPCRs, ion channels, and transporters as well as our own internal whole cell lead generation biology selectivity panel.[1] in vivo: JNJ-63533054 is found to cross the blood-brain barrier and have good drug-like properties amenable for oral dosing in rat. JNJ-63533054 exhibits good stability in both human and rat microsomes and high solubility in aqueous media, and no DDI potential was found. [1] JNJ-63533054 also activates the rat and mouse GPR139 receptor with similar potency (rat EC50 = 63 ± 24 nM, mouse EC50 = 28 ± 7 nM). [2]

Molecular Weight

316.78

Formula

C₁₇H₁₇ClN₂O₂

CAS No.

1802326-66-4

SMILES

O=C(NCC(N[[email protected]](C1=CC=CC=C1)C)=O)C2=CC=CC(Cl)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (157.84 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1568 mL 15.7838 mL 31.5676 mL
5 mM 0.6314 mL 3.1568 mL 6.3135 mL
10 mM 0.3157 mL 1.5784 mL 3.1568 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.89 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.89 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product name:
JNJ-63533054
Cat. No.:
HY-19838
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