PF-06761281
|
|
|
- CAS-Nr.
- 1854061-19-0
- Englisch Name:
- PF-06761281
- Synonyma:
- PF-06761281;PF-06761281 >=97% (HPLC);Butanedioic acid, 2-hydroxy-2-[2-(2-methoxy-5-methyl-3-pyridinyl)ethyl]-, (2R)-
- CBNumber:
- CB04670535
- Summenformel:
- C13H17NO6
- Molgewicht:
- 283.28
- MOL-Datei:
- 1854061-19-0.mol
|
PF-06761281 Eigenschaften
- Siedepunkt:
- 469.7±45.0 °C(Predicted)
- Dichte
- 1.358±0.06 g/cm3(Predicted)
- storage temp.
- -20°C
- pka
- 3.37±0.28(Predicted)
- Aggregatzustand
- powder
- Farbe
- white to beige
- Wasserl?slichkeit
- H2O: 20mg/mL, clear
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
| RIDADR |
UN 2811 6.1 / PGIII |
|
|
| Bildanzeige (GHS) |
|
| Alarmwort |
Achtung |
| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| H301 |
Giftig bei Verschlucken. |
Akute Toxizit?t oral |
Kategorie 3 |
Achtung |
![GHS hazard pictograms]() src="/GHS06.jpg" width="20" height="20" /> |
P264, P270, P301+P310, P321, P330,P405, P501 |
|
| Sicherheit |
|
PF-06761281 Chemische Eigenschaften,Einsatz,Produktion Methoden
Verwenden
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.
Allgemeine Beschreibung
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.
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.
PF-06761281 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
PF-06761281 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 7)Lieferanten
- PF-06761281
- PF-06761281 >=97% (HPLC)
- Butanedioic acid, 2-hydroxy-2-[2-(2-methoxy-5-methyl-3-pyridinyl)ethyl]-, (2R)-
- 1854061-19-0
