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.
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.
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- UPC:
- 51172506
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- Yes
- MPN:
- PZ0318-25MG
- CAS:
- 1854061-19-0
- Temperature Control Device:
- Yes
