PF-06678419
PF-06678419 is a sodium-coupled citrate transporter and sodium-dependent dicarboxylate transporter inhibitor. PF-06678419 inhibits citrate uptake by interacting with residues near and outside NaCT’s citrate binding site. PF-06678419 can be used for the research of type 2 diabetes mellitus.
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- CAS No.: 2055468-48-7
- Formule: C12H13IO5
- Masse moléculaire:364.14
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
PF-06678419 (Compound 4) (30 min) potently inhibits NaCT-mediated citrate uptake in HEK_NaCT cells with an IC50 of 0.44 μM, but lacks selectivity, also inhibiting NaDC1 and NaDC3 with IC50 values of 5.5 μM and 3.2 μM, respectively[1].
PF-06678419 binds to the putative citrate binding site of a human NaCT homology model, with key interactions involving residues G228, V231, V232, and G409[2].
PF-06678419 (10 µM; 12 min) shows altered inhibitory activity against mutant human NaCT-expressing HEK-293 cells, with increased affinity for NaCTQ77K and NaCTV231A mutants, reduced activity against NaCTG228A, NaCTV232A, NaCTV232I, NaCTG409N, and NaCTR481I mutants, and reduced sensitivity (IC50 ≥25 µM) for NaCTG228A and NaCTG409N mutants[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2055468-48-7
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Masse moléculaire 364.14
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Formule C12H13IO5
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SMILES
[C@@](CCC1=CC=C(I)C=C1)(CC(O)=O)(C(O)=O)O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Huard K, et al. Discovery and characterization of novel inhibitors of the sodium-coupled citrate transporter (NaCT or SLC13A5). Sci Rep. 2015;5:17391. Published 2015 Dec 1. [Content Brief]
[2]. Pajor AM, et al. Molecular Basis for Inhibition of the Na+/Citrate Transporter NaCT (SLC13A5) by Dicarboxylate Inhibitors. Mol Pharmacol. 2016;90(6):755-765. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PF-06678419 Related Classifications
HY-124661 Related Classifications
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