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Cat. No.: HY-125011

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JNJ-16567083

Name: JNJ-16567083
Brand: MedChemExpress
SKU: HY-125011
Availability: PreOrder

(Synonyms: EMQMCM free base)

JNJ-16567083 (EMQMCM free base) is a selective, non-competitive metabotropic glutamate receptor 1 (mGluR1) antagonist with a K_i 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

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

JNJ-16567083 Chemical Structure

CAS No.: 852612-00-1

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
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Biological Activity

Description

IC₅₀ & Target

^[2]

mGluR1

0.87 nM (Ki)

All Radionuclide-Drug Conjugates (RDCs) Isoforms :

All mGluR Isoforms :

In Vitro

JNJ-16567083 displays high affinity for the rat mGlu1 receptor (K_i = 0.87 nM) and low affinity for the rat mGlu5 receptor (K_i = 2366 nM) in CHO cells^[1].
JNJ-16567083 is a non-competitive mGluR1 antagonist (K_i = 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.

In Vivo

[¹¹C]JNJ-16567083 (intravenous injection; single injection) exhibited excellent brain uptake, and its binding in the brain was saturable, specific, and selective for mGlu1 receptors, with cold JNJ-16567083 reducing cerebellar specific binding by 81%^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Sprague-Dawley rats (male)^[1]
Dosage:

2 mg/kg (cold JNJ-16567083)
Administration:

i.v.; single injection
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.

Related Protocols :

Human pluripotent stem cell midbrain dopaminergic neuron differentiation

Chemical Information

CAS No. 852612-00-1
Molecular Weight 311.42
Formula C₂₀H₂₅NO₂
SMILES

O=C(C1CCC(CC1)OC)C2=CC3=C(N=C(C)C(CC)=C3)C=C2
Synonyms

EMQMCM free base
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Huang Y, et al. A positron emission tomography radioligand for the in vivo labeling of metabotropic glutamate 1 receptor: (3-ethyl-2-[11C]methyl-6-quinolinyl)(cis- 4-methoxycyclohexyl)methanone. Journal of medicinal chemistry. 2005 Aug 11;48(16):5096-9.

[2]. Sobrio F, et al. Radiosynthesis of carbon-11 and fluorine-18 labelled radiotracers to image the ionotropic and metabotropic glutamate receptors. Journal of labelled compounds & radiopharmaceuticals. 2013;56(3-4):180-6.

[3]. Fuchigami T, et al. Development of PET and SPECT probes for glutamate receptors. TheScientificWorldJournal. 2015;2015:716514.

[4]. Rodriguez P, et al. A Novel Class of Complement 3a Receptor Agonists and Antagonists Derived from the TLQP-21 Peptide. Journal of medicinal chemistry. 2025 Sep 25;68(18):19107-19121. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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JNJ-16567083

All Radionuclide-Drug Conjugates (RDCs) Isoforms

All mGluR Isoforms