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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- 화학식: C19H16ClN7O2
- 분자량:409.83
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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.
[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.
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Animal Model:C57BL/6J (male, 6 months old); GPR39 knockout (male, 6 months old)[1]
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Dosage:8.5 MBq
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Administration:i.v.; single bolus injection
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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.
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Animal Model:APP/PS1 transgenic (male, 6 months old); wild-type (male, 6 months old)[1]
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Dosage:8.5 MBq
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Administration:i.v.; single bolus injection
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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.
Chemical Information
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분자량 409.83
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화학식 C19H16ClN7O2
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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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TMN-OMe Related Classifications
HY-182367 Related Classifications
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