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Products > GPCR > GPR139 > JNJ-63533054
Product name : JNJ-63533054
Item : c2382
Price : 200mg, $750;500mg, $1290; 1g, $1990; 2g, $2995
contact : Send inquiry to: info@acesobio.com
CAS : 1802326-66-4
Molecular Weight : 316.79
Formula : C17H17ClN2O2
Storage : at -20°C
Additional information : We offer significant discount for bulky quantity order.
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Details:
Description of:JNJ-63533054
JNJ 63533054(cas:1802326-66-4)is a potent and selective GPR139 agonist (EC50 = 16 nM) that is brain and cell penetrant. JNJ 63533054 is selective for GPR139 over a panel of GPCRs, ion channels and transporters, including GPR142 and is orally bioavailable.
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).

Quality control data:
Quality control by 1H-NMR, 13C-NMR, HPLC and LCMS.
Product will be shipped with supporting analytical data.

REFERENCES

1: Liu C, Bonaventure P, Lee G, Nepomuceno D, Kuei C, Wu J, Li Q, Joseph V, Sutton SW, Eckert W, Yao X, Yieh L, Dvorak C, Carruthers N, Coate H, Yun S, Dugovic C, Harrington A, Lovenberg TW. 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. 2015 Nov;88(5):911-25. doi: 10.1124/mol.115.100412. Epub 2015 Sep 8. PubMed PMID: 26349500.

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