PF-06649298_product_DataBase

Bioactivity	PF-06649298 is a sodium-coupled citrate transporter (NaCT or SLC13A5) inhibitor. PF-06649298 specifically interacts with NaCT with an IC50 value of 16.2 μM to inhibits the transport of citrate in human hepatocytes. PF-06649298 can be used for the research of regulating glucose metabolism and lipid metabolism[1][2].
Target	IC50: 408 nM (citrate uptake in HEKNaCT), 16.2 μM (citrate uptake in Human Heps), 4.5 μM (citrate uptake in Mouse Heps), ＞100 μM (citrate uptake in HEKNaCD1), ＞100 μM (citrate uptake in HEKNaCD3)
Invitro	PF-06649298 (0-100 μM; 30 min) inhibits citrate uptaken in cells[1]. Cell Viability Assay[1] Cell Line:
In Vivo	PF-06649298 (250 mg/kg; p.o. twice a day; for 21 days) reverses glucose intolerance of high fat diet (HFD) mice[2]. Animal Model:
Name	PF-06649298
CAS	1854061-16-7
Formula	C16H22O5
Molar Mass	294.34
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Huard K, et al. Optimization of a Dicarboxylic Series for in Vivo Inhibition of Citrate Transport by the Solute Carrier 13 (SLC13) Family. J Med Chem. 2016 Feb 11;59(3):1165-75. [2]. Huard K, et al. Discovery and characterization of novel inhibitors of the sodium-coupled citrate transporter (NaCT or SLC13A5). Sci Rep. 2015 Dec 1;5:17391.

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