Volume 20, Issue 4 p. A266-A266
Pharmacology (American Society for Pharmacology and Experimental Therapeutics)
Free Access

BLX-1028, an orally active small molecules having anti-adipogenic property, reduces weight gain, fat content and improves glucose tolerance in Diet Induced Obesity model in mice

Abhijeet Nag

Abhijeet Nag

Research & Development, BEXEL Pharmaceuticals Inc., 32990 Alvarado Niles Rd., Suite 910, Union City, CA, 94587

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Shyamali Roy

Shyamali Roy

Research & Development, BEXEL Pharmaceuticals Inc., 32990 Alvarado Niles Rd., Suite 910, Union City, CA, 94587

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Hyang Moon

Hyang Moon

Research & Development, BEXEL Pharmaceuticals Inc., 32990 Alvarado Niles Rd., Suite 910, Union City, CA, 94587

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Ananda Sen

Ananda Sen

Research & Development, BEXEL Pharmaceuticals Inc., 32990 Alvarado Niles Rd., Suite 910, Union City, CA, 94587

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Partha Neogi

Partha Neogi

Research & Development, BEXEL Pharmaceuticals Inc., 32990 Alvarado Niles Rd., Suite 910, Union City, CA, 94587

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Deben Dey

Deben Dey

Research & Development, BEXEL Pharmaceuticals Inc., 32990 Alvarado Niles Rd., Suite 910, Union City, CA, 94587

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Bishwajit Nag

Bishwajit Nag

Research & Development, BEXEL Pharmaceuticals Inc., 32990 Alvarado Niles Rd., Suite 910, Union City, CA, 94587

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First published: 06 March 2006

Abstract

BLX-1028 is a water soluble, orally active, modified amino acid conjugated small molecule with no structural resemblance with any existing anti-obesity compounds. BLX-1028 showed a dose dependent inhibition of adipocyte differentiation at 0.1mM (30.4%), 1mM (40.2%) and 10mM (99.2%) concentrations in 3T3-L1 cells when incubated along with rosiglitazone (1mM), a known PPARy agonist. In Diet Induced Obesity Model (DIO), where obesity was induced in C57BL/6 mice by feeding on a high fat (60% fat) diet, treatment with BLX-1028 at 5, 50 and 100 mg/kg/day, lowered body weight gain by 40 % in comparison to vehicle treated animals. No significant changes in food and water intake were observed. In a dual-energy X-ray absorptiometry (DXA) technique with an image analysis procedure, it showed reduction in body fat content in treatment group compare to vehicle. Oral glucose tolerance test performed on days 0, 30, 60 and 90 showed an improvement in glucose tolerance. No significant changes were observed in cholesterol, triglyceride and free fatty acid levels. Blood serum analysis after 30, 60 and 90 days of treatment revealed that no significant difference in AST and ALT levels. The mechanism of action of BLX-1028 is currently being investigated. These results combined demonstrate the potential of BLX-1028 as a novel compound for the treatment of obesity and related disorders.