CP 91,149 – 10 mg

Brand:
Cayman
CAS:
186392-40-5
Storage:
-20
UN-No:
Non-Hazardous - /

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).{41399,41400,41401} CP 91,149 is 5- to 10-fold less potent in the absence of glucose.{41399} 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.{41399,41401} 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.{41402} 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.{41399}  

 

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Description

An inhibitor of LGPa, MGPa, and MGPb (IC50s = 0.13, 0.2, and 0.3 μM, respectively, in the presence of glucose); 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; inhibits brain GP (IC50 = 0.5 μM) and glycogen accumulation and proliferation of A549 NSCLC cells that express endogenous brain GP (30 μM); lowers 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 (25 mg/kg, p.o.)


Formal name: 5-chloro-N-[(1S,2R)-3-(dimethylamino)-2-hydroxy-3-oxo-1-(phenylmethyl)propyl]-1H-indole-2-carboxamide

Synonyms: 

Molecular weight: 399.9

CAS: 186392-40-5

Purity: ≥98%

Formulation: A crystalline solid


Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Metabolism||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes