JNJ-16567083
JNJ-16567083 (EMQMCM free base) is a selective, non-competitive metabotropic glutamate receptor 1 (mGluR1) antagonist with a Ki value of 0.87 nM. JNJ-16567083 can be radiolabeled to serve as a PET radiotracer. JNJ-16567083 can be used for research on Parkinson's disease and asthma.
For research use only. We do not sell to patients.
- CAS No.: 852612-00-1
- Formula: C20H25NO2
- Molecular Weight:311.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
All Radionuclide-Drug Conjugates (RDCs) Isoforms
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Biological Activity
Description
IC50 & Target
[2]|
mGluR1 0.87 nM (Ki) |
In Vitro
JNJ-16567083 displays high affinity for the rat mGlu1 receptor (Ki = 0.87 nM) and low affinity for the rat mGlu5 receptor (Ki = 2366 nM) in CHO cells[1].
JNJ-16567083 is a non-competitive mGluR1 antagonist (Ki = 0.87 nM) that was successfully radiolabelled via Stille coupling, though no further applications were published[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley rats (male)[1]
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Dosage:2 mg/kg (cold JNJ-16567083)
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Administration:i.v.; single injection
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Result:Initial uptake of [11C]2 in the brain was high, with %ID/g ranging from 0.47% in the medulla to 1.24% in the cerebellum at 10 min after radioligand injection.
The ratio of radioactivity in the cerebellum to that in the medulla was 2.63, 4.72, and 4.06 at 10, 30, and 60 min, respectively.
When rats were pretreated with cold compound JNJ-16567083 (2 mg/kg, i.v.) 10 min before radioligand injection and sacrificed 30 min after, specific binding of the radioligand in the cerebellum was reduced by 81% compared with the control group.
Chemical Information
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CAS No. 852612-00-1
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Molecular Weight 311.42
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Formula C20H25NO2
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SMILES
O=C(C1CCC(CC1)OC)C2=CC3=C(N=C(C)C(CC)=C3)C=C2
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Synonyms
EMQMCM free base
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Human pluripotent stem cell midbrain dopaminergic neuron differentiation
Human pluripotent stem cells are directed toward midbrain dopaminergic neurons by first inducing a neural floor-plate-like progenitor state, then patterning cells with ventralizing SHH signaling and midbrain/WNT-FGF cues, and finally maturing progenitors into neurons expressing dopaminergic markers such as TH, NURR1/NR4A2, PITX3, DAT/SLC6A3, VMAT2/SLC18A2, GIRK2/KCNJ6, FOXA2, LMX1A, and EN1. The main readouts are loss of pluripotency, acquisition of FOXA2+/LMX1A+ midbrain floor-plate progenitors, emergence of βIII-tubulin+/MAP2+ neurons, and production of TH+ dopaminergic neurons with molecular, dopamine-release, and electrophysiological features of midbrain dopaminergic identity.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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