PZ0318
PF-06761281
≥97% (HPLC)
Synonym(s):
(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
Sign In to View Organizational & Contract Pricing.
Select a Size
Change View
About This Item
Empirical Formula (Hill Notation):
C13H17NO6
CAS Number:
Molecular Weight:
283.28
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12161503
MDL number:
Quality Level
assay
≥97% (HPLC)
form
powder
color
white to beige
solubility
H2O: 20 mg/mL, clear
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
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.
signalword
Danger
hcodes
Hazard Classifications
Acute Tox. 3 Oral
Storage Class
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Choose from one of the most recent versions:
Already Own This Product?
Find documentation for the products that you have recently purchased in the Document Library.
Determination of Unbound Partition Coefficient and in Vitro-in Vivo Extrapolation for SLC13A Transporter-Mediated Uptake.
Riccardi K et al
Drug Metabolism and Disposition, 44(10), 1633-1642 (2016)
Kim Huard et al.
Journal of medicinal chemistry, 59(3), 1165-1175 (2016-01-07)
Inhibition of the sodium-coupled citrate transporter (NaCT or SLC13A5) has been proposed as a new therapeutic approach for prevention and treatment of metabolic diseases. In a previous report, we discovered dicarboxylate 1a (PF-06649298) which inhibits the transport of citrate in
Global Trade Item Number
| SKU | GTIN |
|---|---|
| PZ0318-5MG | 04061832575612 |
| PZ0318-25MG | 04061832575605 |