GPCR modulator-1
GPCR modulator-1 is a negative allosteric modulator of the GLP-1 receptor (GLP-1R). GPCR modulator-1 can be used for the study of type 2 diabetes.
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- No. CAS: 1407592-99-7
- Fòrmula: C26H28F3N5O3
- Peso molecular:515.53
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
Actividad biológica
Descripciòn
In Vitro
GPCR modulator-1 (PF-06372222) can effectively inhibit the cAMP accumulation caused by GLP-1 stimulation in HEK-293T cells expressing wild-type GLP-1R. Its pIC50 value is 5.15. After mutations at C347 and I328, its efficacy is enhanced, with pIC50 values of 5.97 and 5.55, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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No. CAS 1407592-99-7
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Peso molecular 515.53
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Fòrmula C26H28F3N5O3
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SMILES
O=C(O)CCNC(C1=CC=C([C@@H](C2CC(C)(C)C2)NC3=CC=C(N4C=C(C(F)(F)F)N=C4)N=C3)C=C1)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocolo
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)