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PF-01247324

PF-01247324 Struktur
875051-72-2
CAS-Nr.
875051-72-2
Englisch Name:
PF-01247324
Synonyma:
133786;CS-2577;PF-1247324;PF-01247324;PF01247324;PF 01247324;6-amino-N-methyl-5-(2,3,5-trichlorophenyl)picolinamide;6-AMINO-N-METHYL-5-(2,3,5-TRICHLOROPHENYL)PYRIDINE-2-CARBOXAMIDE;2-PyridinecarboxaMide, 6-aMino-N-Methyl-5-(2,3,5-trichlorophenyl)-;6-AMINO-5-(2,3,5-TRICHLORO-PHENYL)-PYRIDINE-2-CARBOXYLIC ACID METHYLAMIDE;Sodium Channel,PF 01247324,PF-01247324,Na+ channels,Na channels,PF01247324,Inhibitor,inhibit
CBNumber:
CB42682530
Summenformel:
C13H10Cl3N3O
Molgewicht:
330.6
MOL-Datei:
875051-72-2.mol

PF-01247324 Eigenschaften

Siedepunkt:
477.7±45.0 °C(Predicted)
Dichte
1.460±0.06 g/cm3(Predicted)
storage temp. 
room temp
L?slichkeit
DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 30 mg/ml; Ethanol:PBS (pH 7.2) (1:4): 0.2 mg/ml
pka
6.56±0.46(Predicted)
Aggregatzustand
powder
Farbe
white to beige
Sicherheit
  • Risiko- und Sicherheitserkl?rung
  • Gefahreninformationscode (GHS)
RIDADR  UN 2811 6.1 / PGIII
Bildanzeige (GHS) GHS hazard pictograms
Alarmwort Achtung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H301 Giftig bei Verschlucken. Akute Toxizit?t oral Kategorie 3 Achtung GHS hazard pictogramssrc="/GHS06.jpg" width="20" height="20" /> P264, P270, P301+P310, P321, P330,P405, P501
H315 Verursacht Hautreizungen. Hautreizung Kategorie 2 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P280, P302+P352, P321,P332+P313, P362
H319 Verursacht schwere Augenreizung. Schwere Augenreizung Kategorie 2 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P280, P305+P351+P338,P337+P313P
H335 Kann die Atemwege reizen. Spezifische Zielorgan-Toxizit?t (einmalige Exposition) Kategorie 3 (Atemwegsreizung) Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" />
Sicherheit
P302+P352 BEI BERüHRUNG MIT DER HAUT: Mit viel Wasser/... (Hersteller kann, falls zweckm??ig, ein Reinigungsmittel angeben oder, wenn Wasser eindeutig ungeeignet ist, ein alternatives Mittel empfehlen) waschen.
P305+P351+P338 BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach M?glichkeit entfernen. Weiter spülen.

PF-01247324 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

PF-01247324 is a blocker of the tetrodotoxin-resistant (TTX-R) sodium channel Nav1.8 (IC50 = 0.19 μM for human Nav1.8). It is selective for Nav1.8 over Nav1.1, Nav1.2, Nav1.5, and Nav1.7 channels (IC50s = 13, 12.8, 9, and 19 μM, respectively) as well as ether-a-go-go (ERG) potassium channels (IC50 = 30 μM). PF-01247324 blocks Nav1.8 channels in a VSP-FRET assay using HEK293 cells (IC50 = 2.6 μM). In vivo, PF-01247324 (100 mg/kg) reduces phase 2 flinching in a rat model of formalin-induced persistent pain. It increases latency to lift the inflamed paw and latency to paw withdrawal in rat models of carrageenan-induced thermal hyperalgesia and mechanical hyperalgesia induced by complete Freund''s adjuvant (CFA), respectively.

Biochem/physiol Actions

In humans, PF-01247324 [6-amino-5-(2, 3, 5-trichloro-phenyl)-pyridine-2-carboxylic acid methylamide] prevents native tetrodotoxin-resistant (TTX-R) currents in dorsal root ganglion (DRG) neurons.

Enzyminhibitor

This novel oral NaV1.8 blocker (FW = 330.59 g/mol) attenuates nociception and neuronal excitability by selectively targeting voltage-gated sodium transporter NaV1.8, with much weaker action against NaV1.1, NaV1.2, NaV1.4, NaV1.5, NaV1.6, and NaV1.7 transporters. PF-01247324 inhibited native tetrodotoxin-resistant (TTX-R) currents in human dorsal root ganglion (DRG) neurons (IC50 = 331 nM) and in recombinantly expressed hNav 1.8 (IC50 = 196 nM), with 50-fold selectivity over recombinantly expressed TTX-R hNav 1.5 channels (IC50 ～ 10 μM) and 65-100 greater selectivity over TTX-sensitive (TTX-S) channels (IC50 ～ 10-18 μM). Native TTX-R currents in small diameter rodent DRG neurons were inhibited with an IC50 of 448 nM, and the block of both human recombinant Nav1.8 and TTX-R from rat DRG neurons was both frequency and statedependent. Unlike previously published NaV1.8 blockers, PF-01247324 demonstrates frequency-dependence, and off-target frequency-dependence at other sodium channel subtypes may reduce its selectivity window. The majority of small molecule sodium channel blockers interact at the local anesthetic binding site, which due to a high level of sequence homology across voltage-gated sodium channel subtypes seems an unlikely site for interaction of selective agents such as PF-01247324. The majority of small molecule sodium channel blockers interact at the local anesthetic binding site, which due to a high level of sequence homology across voltage-gated sodium channel subtypes seems an unlikely site for interaction of selective agents such as PF-01247324

PF-01247324 Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

PF-01247324 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 50)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
ATK CHEMICAL COMPANY LIMITED 		+undefined-21-51877795
ivan@atkchemical.com China 32956 60
TargetMol Chemicals Inc. 		+1-781-999-5354 +1-00000000000
 marketing@targetmol.com United States 32161 58
InvivoChem 		+1-708-310-1919 +1-13798911105
 sales@invivochem.cn United States 6391 58
TargetMol Chemicals Inc.
support@targetmol.com United States 38631 58
ShenZhen Trendseen Biological Technology Co.,Ltd. 		13417589054
 trendseenbio@gmail.com China 11681 58
Amadis Chemical Company Limited 		571-89925085
sales@amadischem.com China 131957 58
ChemShuttle, Inc. 0510-83588313-802 18800520310;
 sales@chemshuttle.com China 3002 62
Modachem Shanghai Co., Ltd +86 (0)21 51320687 51371369 1744605818
China 1578 58
Sigma-Aldrich 021-61415566 800-8193336
 orderCN@merckgroup.com China 51456 80
Shanghai Lollane Biological Technology Co.,Ltd. 021-52996696，15000506266 15000506266
 China 4575 55

875051-72-2()Verwandte Suche:

  • 2-PyridinecarboxaMide, 6-aMino-N-Methyl-5-(2,3,5-trichlorophenyl)-
  • 6-amino-N-methyl-5-(2,3,5-trichlorophenyl)picolinamide
  • 6-AMINO-5-(2,3,5-TRICHLORO-PHENYL)-PYRIDINE-2-CARBOXYLIC ACID METHYLAMIDE
  • PF-1247324
  • PF-01247324
  • 6-AMINO-N-METHYL-5-(2,3,5-TRICHLOROPHENYL)PYRIDINE-2-CARBOXAMIDE
  • PF01247324;PF 01247324
  • 133786
  • CS-2577
  • Sodium Channel,PF 01247324,PF-01247324,Na+ channels,Na channels,PF01247324,Inhibitor,inhibit
  • 875051-72-2
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