2. GPCR/G Protein
  3. GPR39
  4. TMN-OMe

TMN-OMe is a blood-brain barrier-permeable GPR39 agonist and a radiotracer for positron emission tomography (PET). TMN-OMe activates GPR39 by recruiting β-arrestin, exhibits highly selective binding ability in the mouse brain, and enables quantitative analysis of GPR39 at the in vivo level. TMN-OMe shows specific uptake in GPR39 knockout mice, Alzheimer's disease model (APP/PS1) mice, and blocking experiments. TMN-OMe facilitates in-depth exploration of changes in GPR39-related mechanisms in neurological diseases and is widely used in Alzheimer's disease research.

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TMN-OMe

TMN-OMe Chemical Structure

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TMN-OMe Related Antibodies

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Description

TMN-OMe is a blood-brain barrier-permeable GPR39 agonist and a radiotracer for positron emission tomography (PET). TMN-OMe activates GPR39 by recruiting β-arrestin, exhibits highly selective binding ability in the mouse brain, and enables quantitative analysis of GPR39 at the in vivo level. TMN-OMe shows specific uptake in GPR39 knockout mice, Alzheimer's disease model (APP/PS1) mice, and blocking experiments. TMN-OMe facilitates in-depth exploration of changes in GPR39-related mechanisms in neurological diseases and is widely used in Alzheimer's disease research[1].

In Vitro

TMN-OMe (5 nM-33.3 μM; 2 h) activates human GPR39 expressed in CHO-K1 cells with an EC50 of 1.65 μM in a β-arrestin recruitment assay[1].

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

TMN-OMe Related Antibodies
In Vivo

[11C]TMN-OMe (8.5 MBq; i.v.; single bolus injection) exhibits rapid blood-brain barrier penetration and specific binding to GPR39 in healthy male BALB/c mice, with baseline brain SUV of 0.31 g/mL that is reduced by up to 86.8% under blocking conditions[1].
[11C]TMN-OMe (8.5 MBq; i.v.; single bolus injection) detects reduced GPR39 levels in the brains of APP/PS1 Alzheimer's disease model mice[1].

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

Animal Model: C57BL/6J (male, 6 months old); GPR39 knockout (male, 6 months old)[1]
Dosage: 8.5 MBq
Administration: i.v.; single bolus injection
Result: Reached brain uptake of 0.31 g/mL SUV in wild-type mice versus 0.09 g/mL SUV in GPR39 knockout mice, representing a 69.4% decrease.
Showed brain uptake of 1.01 %ID/g in wild-type mice versus 0.29 %ID/g in GPR39 knockout mice at 30 min postinjection, a 71% reduction.
Demonstrated wild-type brain uptake of 6.35 PSL/mm2 versus 4.58 PSL/mm2 in GPR39 knockout mice via ex vivo autoradiography, a 27% decrease.
Animal Model: APP/PS1 transgenic (male, 6 months old); wild-type (male, 6 months old)[1]
Dosage: 8.5 MBq
Administration: i.v.; single bolus injection
Result: Reached brain uptake of 0.15 g/mL SUV in APP/PS1 mice versus 0.29 g/mL SUV in wild-type mice, representing a 46.8% decrease.
Molecular Weight

409.83

Formula

C19H16ClN7O2
SMILES

CC1=NN(C(N2)=C1C(C3=C(Cl)C=C(OC)C=C3)CC2=O)C4=NC=NC5=C4N=CN5
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TMN-OMe Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TMN-OMeGPR39human serumalzheimer's diseasehuman GPR39mouse brainAPP/PS1 miceβ-arrestinGPR39 knockout miceBALB/c miceCHO-K1 cellsInhibitorinhibitorinhibit

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