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Cat. No.: HY-124661

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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
화학식: C₁₂H₁₃IO₅
분자량:364.14

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Please store the product under the recommended conditions in the Certificate of Analysis.

PF-06678419 Chemical Structure

CAS No.: 2055468-48-7

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
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- In Vitro
Chemical Information
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Biological Activity

제품 설명

All Sodium Channel Isoforms :

In Vitro

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 NaCT^Q77K and NaCT^V231A mutants, reduced activity against NaCT^G228A, NaCT^V232A, NaCT^V232I, NaCT^G409N, and NaCT^R481I mutants, and reduced sensitivity (IC₅₀ ≥25 µM) for NaCT^G228A and NaCT^G409N mutants^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 2055468-48-7
분자량 364.14
화학식 C₁₂H₁₃IO₅
SMILES

[C@@](CCC1=CC=C(I)C=C1)(CC(O)=O)(C(O)=O)O
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Handling Instructions (2659 KB)

References

[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]

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
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PF-06678419

All Sodium Channel Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

PF-06678419 Related Classifications

HY-124661 Related Classifications