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Submit ReviewJNJ 63533054 is a potent and selective GPR139 agonist (EC50 = 16 nM). Selective for GPR139 over a panel of GPCRs, ion channels and transporters, including GPR142. Brain and cell penetrant. Orally bioavailable.
JNJ 63533054 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
M. Wt | 316.78 |
Formula | C17H17ClN2O2 |
Storage | Store at RT |
Purity | ≥98% (HPLC) |
CAS Number | 1802326-66-4 |
PubChem ID | 2548547 |
InChI Key | MWDVCHRYCKXEBY-LBPRGKRZSA-N |
Smiles | O=C(CNC(C1=CC=CC(Cl)=C1)=O)N[C@@H](C)C2=CC=CC=C2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 31.68 | 100 | |
ethanol | 6.34 | 20 |
The following data is based on the product molecular weight 316.78. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 3.16 mL | 15.78 mL | 31.57 mL |
5 mM | 0.63 mL | 3.16 mL | 6.31 mL |
10 mM | 0.32 mL | 1.58 mL | 3.16 mL |
50 mM | 0.06 mL | 0.32 mL | 0.63 mL |
References are publications that support the biological activity of the product.
Dvorak et al (2015) Identification and SAR of glycine benzamides as potent agonists for the GPR139 receptor. ACS Med.Chem.Lett. 6 1015 PMID: 26396690
If you know of a relevant reference for JNJ 63533054, please let us know.
Keywords: JNJ 63533054, JNJ 63533054 supplier, JNJ63533054, GPR139, agonists, agonism, potent, selective, orally, available, brain, penetrant, orphan, 7-TM, receptors, Orphan, Receptors, 5666, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for JNJ 63533054 include:
Susumu et al (2021) Gene-environment interactions mediate stress susceptibility and resilience through the CaMKIIβ/TARPγ-8/AMPAR pathway. iScience 24 102504 PMID: 34113835
Do you know of a great paper that uses JNJ 63533054 from Tocris? Please let us know.
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