CP 91149

Bezeichnung:CP 91149

CAS-Nr186392-40-5

Englisch Name:CP 91149

CBNumberCB22543734

SummenformelC21H21ClN3O3

Molgewicht398.86274

MOL-Datei186392-40-5.mol

CP 91149 physikalisch-chemischer Eigenschaften

Schmelzpunkt	190-192°C
storage temp.	2-8°C
Löslichkeit	DMSO: >20mg/mL
Aggregatzustand	powder
Farbe	white to off-white
Stabilität	Hygroscopic

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	22
WGK Germany	3

Gefahreninformationscode (GHS)

CP 91149 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
CP 91,149 is an inhibitor of human liver glycogen phosphorylase a (LGPa), muscle glycogen phosphorylase a (MGPa), and MGPb (IC₅₀s = 0.13, 0.2, and 0.3 μM, respectively, in the presence of glucose). CP 91,149 is 5- to 10-fold less potent in the absence of glucose. In vitro, it inhibits glucagon-stimulated glycogenolysis in primary human hepatocytes (IC₅₀ = 2.1 μM) and increases glycogen synthesis in rat hepatocytes at a concentration of 2.5 μM in the presence of 5 mM glucose. CP 91,149 inhibits brain GP (IC₅₀ = 0.5 μM) and, at a concentration of 30 μM, inhibits glycogen accumulation and proliferation of A549 non-small cell lung carcinoma (NSCLC) cells that express endogenous brain GP. In vivo, CP 91,149 (25 mg/kg, p.o.) lowers the plasma glucose level in diabetic ob/ob mice within 3 hours of administration without producing hypoglycemia, but has no effect on normoglycemic, non-diabetic mice.
Chemische Eigenschaften
White Solid
Verwenden
Inhibition of glycogen phosphorylase (GP) by CP-91,149 induces growth inhibition correlating with brain GP expression. Antitumor agent.
Biochem/physiol Actions
CP-91149 is a selective glycogen phosphorylase inhibitor.
in vitro
cp-91149 treatment suppressed glycogenolysis stimulated by glucagon in in primary human hepatocytes and isolated rat hepatocytes with ic50 value of 2.1 μm and 10–100 μm, respectively 1. inhibition of phosphorylase a by cp-91149 resulted in activation of glycogen synthase and translocation of the protein from a soluble to a particulate fraction, which mimicked the insulin- stimulated glycogen synthesis 2.
in vivo
treatment of cp-91149 on diabetic ob/ob mice at a dosage of 25–50 mg/kg was shown to lead to a rapid glucose lowering but did not change glucose levels in normoglycemic, nondiabetic mice 1.
target
GP
Einzelnachweise
1. martin wh, hoover dj, armento sj, et al. discovery of a human liver glycogen phosphorylase inhibitor that lowers blood glucose in vivo. proceedings of the national academy of sciences of the united states of america. 1998;95(4):1776-1781.2. aiston s, coghlan mp, agius l. inactivation of phosphorylase is a major component of the mechanism by which insulin stimulates hepatic glycogen synthesis. european journal of biochemistry / febs. 2003;270(13):2773-2781.

CP 91149 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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