2. 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.

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GPR3 inverse agonist-1 TFA

GPR3 inverse agonist-1 TFA Chemical Structure

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GPR3 inverse agonist-1 TFA Related Antibodies

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Description

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[1].

In Vitro

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.

GPR3 inverse agonist-1 TFA Related Antibodies
Parmacokinetics
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 %
Molecular Weight

391.39

Formula

C20H20F3N3O2
SMILES

N=C1N(CC2=CC=CC=C2)C3=CC=CC=C3N1CC4CC4.O=C(O)C(F)(F)F
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
References
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GPR3 inverse agonist-1 TFA 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:

GPR3 inverse agonist-1alzheimer's diseaseGPR12GPR3HEK293A cellsGPR6Inhibitorinhibitorinhibit

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