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PF-06761281

SIGMA/PZ0318 - ≥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
Linear Formula: C13H17NO6
Product Type: Chemical
Catalog Number PKG Qty. Price Quantity
45-PZ0318-5MG 5 mg
 $119.00
1/EA		 Add To Favorites
45-PZ0318-25MG 25 mg
 $480.00
1/EA		 Add To Favorites

 

assay ≥97% (HPLC)
color white to beige
form powder
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
Quality Level 100 
shipped in dry ice
SMILES string CC1=CC(CC[C@](CC(O)=O)(O)C(O)=O)=C(OC)N=C1
solubility H2O: 20 mg/mL, clear
storage temp. −20°C
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.
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.
Packaging: 5, 25 mg in glass bottle
Symbol GHS06  GHS06
Signal word Danger
Hazard statements H301
Precautionary statements P301 + P330 + P331 + P310
RIDADR UN 2811 6.1 / PGIII
WGK Germany WGK 3
Flash Point(F) Not applicable
Flash Point(C) Not applicable
Purity ≥97% (HPLC)
Storage Temp. −20°C
UNSPSC 12161503

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