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PZ0318 Sigma-Aldrich

PF-06761281

≥97% (HPLC)

Synonym: (2R)-2-Hydroxy-2-[2-(2-methoxy-5-methyl-3-pyridinyl)ethyl]-butanedioic acid, (R)-2-Hydroxy-2-(2-(2-methoxy-5-methylpyridin-3-yl)ethyl)-succinic acid

  • CAS Number 1854061-19-0

  • Empirical Formula (Hill Notation) C13H17NO6

  • Molecular Weight 283.28

  •  MDL number MFCD30187578

  •  PubChem Substance ID 329823836

  •  NACRES NA.77

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Properties

Related Categories Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience, Ion Channels,
Quality Level   100
assay   ≥97% (HPLC)
form   powder
mfr. no.   Pfizer®
color   white to beige
solubility   H2O: 20 mg/mL, clear
originator   Pfizer
shipped in   dry ice
storage temp.   −20°C
SMILES string   CC1=CC(CC[C@](CC(O)=O)(O)C(O)=O)=C(OC)N=C1
InChI   1S/C13H17NO6/c1-8-5-9(11(20-2)14-7-8)3-4-13(19,12(17)18)6-10(15)16/h5,7,19H,3-4,6H2,1-2H3,(H,15,16)(H,17,18)/t13-/m1/s1
InChI key   FGYMJXFSHBLHLW-CYBMUJFWSA-N

Description

General description

PF-06761281 is a small, polar dicarboxylate compound. Its structure is similar to citrate, which is the endogenous substrate of Na+-citrate cotransporter (NaCT). It is a novel, potent inhibitor of SLC13a2/3/5 (solute channel) family, along with selectivity for NaCT.

Application

PF-06761281 has been used as a SLC13A family inhibitor, in rats to determine its unbound partition coefficient (Kpuu), to estimate its potency as a drug.

Packaging

5, 25 mg in glass bottle

Biochem/physiol Actions

PF-06761281 is an inhibitor of the sodium-coupled citrate transporter (NaCT or SLC13A5), which may be a target for tretment and prevention of metabolic disorders. The SLC13 transporters SLC13A2 (NaDC1), SLC13A3 (NaDC3), and SLC13A5 (NaCT) co-transport di- and tricarboxylates with multiple sodium ions into cells. PF-06761281 inhibits citrate uptake with an IC50 of 740 nM for NaCT in human hepatocytes. PF-06761281 has >25-fold in vitro selectivity for NaCT over NaDC1 and NaDC3 and was inactive in a selectivity panel of 65 targets.

Other Notes

This compound was developed by Pfizer for Ion Channel research. To learn more about Sigma′s partnership with Pfizer and view other authentic, high-quality Pfizer compounds, visit sigma.com/bsm-pfizer.

Legal Information

Sold for research purposes under agreement from Pfizer Inc.

Pfizer is a registered trademark of Pfizer, Inc.

Safety & Documentation

Safety Information

Symbol 
GHS06  GHS06
Signal word 
Danger
Hazard statements 
Precautionary statements 
RIDADR 
UN 2811 6.1 / PGIII
WGK Germany 
WGK 3
Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable

Documents

Certificate of Analysis (COA)

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Protocols & Articles

Articles

Pfizer Compounds for Ion Channels

From our library of Articles, Sigma-Aldrich presents Pfizer Compounds for Ion Channels

Peer-Reviewed Papers
15

References

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