GPR3 inverse agonist-1 TFA
GPR3 inverse agonist-1 TFA is a selective and competitive GPR3 inverse agonist with an EC50 of 5 μM. GPR3 inverse agonist-1 TFA inhibits GPR3-dependent Gs activity, stabilizes a specific receptor conformation, and reduces cAMP levels. GPR3 inverse agonist-1 TFA can be used for the research of Alzheimer's disease.
For research use only. We do not sell to patients.
- Formula: C20H20F3N3O2
- Molecular Weight:391.39
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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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
GPR3 inverse agonist-1 TFA (Compound 33) (0.01-100 μM) induces GPR3-specific conformational changes in stably transfected HEK293A cells with an EC50 of 5 μM[1].
GPR3 inverse agonist-1 TFA (0.01-100 μM) acts as a GPR3 inverse agonist in HEK293A cells expressing the Gs dissociation biosensor, with an EC50 of 250 nM[1].
GPR3 inverse agonist-1 TFA (0.01-100 μM) reduces cAMP levels in GPR3-expressing HEK293A cells with an EC50 of 2 μM, showing selectivity over GPR6 and GPR12 receptors[1].
GPR3 inverse agonist-1 TFA competes with the agonist DPI (HY-100965) for binding to GPR3 in HEK293A cells, but does not interfere with the binding of the inverse agonist AF64394 (HY-12664)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | AUC0-t | AUC0-∞ | MRT0-∞ | T1/2 | Tmax | Cmax | CL | F |
|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 2 mg/kg | i.v. | 5380 ng·h/mL | 5400 ng·h/mL | 0.60 h | 1.20 h | 0.083 h | 12100 ng/mL | 374 mL/h/kg | / |
| Rat[1] | 2 mg/kg | i.v. | 5380 ng·h/mL | 5400 ng·h/mL | 0.60 h | 1.20 h | 0.083 h | 12100 ng/mL | 374 mL/h/kg | / |
| Rat[1] | 2 mg/kg | i.v. | 5380 ng·h/mL | 5400 ng·h/mL | 0.60 h | 1.20 h | 0.083 h | 12100 ng/mL | 374 mL/h/kg | / |
| Rat[1] | 20 mg/kg | p.o. | 18100 ng·h/mL | 18200 ng·h/mL | 3.20 h | 1.70 h | 2.33 h | 4930 ng/mL | / | 33.71 % |
| Rat[1] | 20 mg/kg | p.o. | 18100 ng·h/mL | 18200 ng·h/mL | 3.20 h | 1.70 h | 2.33 h | 4930 ng/mL | / | 33.71 % |
| Rat[1] | 20 mg/kg | p.o. | 18100 ng·h/mL | 18200 ng·h/mL | 3.20 h | 1.70 h | 2.33 h | 4930 ng/mL | / | 33.71 % |
Chemical Information
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Molecular Weight 391.39
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Formula C20H20F3N3O2
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SMILES
N=C1N(CC2=CC=CC=C2)C3=CC=CC=C3N1CC4CC4.O=C(O)C(F)(F)F
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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