Holiday Notification: Cayman Chemical will be closed Monday, May 28, 2012, in observance of the Memorial Day holiday.
More…
Please feel free to continue placing orders via our website or via fax at 734-971-3640. You may send an email to customer service at custserv@caymanchem.com , or to technical support at techserv@caymanchem.com which we will respond to the next business day. Cayman will resume regular business hours and shipping schedules on Tuesday, May 29, 2012. Thank you for your patience and understanding.
Stearoyl-CoA desaturase (SCD) catalyzes the committed step of the conversion of saturated, long-chain fatty acids to monounsaturated fatty acids. The SCD1 gene is thought to play a key role in lipid homeostasis and body weight regulation.1,2,3 Thus, modulating SCD1 activity pharmacologically may be a useful tool for regulating type 2 diabetes, dyslipidemia, and obesity. CAY10566 is a potent and selective inhibitor of SCD1 that demonstrates IC50 values of 4.5 and 26 nM in mouse and human enzymatic assays, respectively.4 This compound inhibits the conversion of saturated, long-chain fatty acyl-CoAs to monounsaturated, long-chain fatty acyl-CoAs in Hep-G2 cells with IC50 values of 7.9 and 6.8 nM, respectively, when heptadecanoic acid and palmitic acid are used as the substrate.4
1
Cohen, P., Miyazaki, M., Socci, N.D., et al. Role for stearoyl-CoA desaturase-1 in leptin-mediated weight loss. Science297240-243(2002).
2
Dobrzyn, P., Sampath, H., Dobrzyn, A., et al. Loss of stearoyl-CoA desaturase 1 inhibits fatty acid oxidation and increases glucose utilization in the heart. Am J Physiol Endocrinol Metab294E357-E364(2008).
3
Miyazaki, M., Flowers, M.T., Sampath, H., et al. Hepatic stearoyl-CoA desaturase-1 deficiency protects mice from carbohydrate-induced adiposity and hepatic steatosis. Cell Metab6484-496(2007).
4
Liu, G., Lynch, J.K., Freeman, J., et al. Discovery of potent, selective, orally bioavailable stearoyl-CoA desaturase 1 inhibitors. J Med Chem503086-3100(2007).
Room temperature
in continental US; may vary elsewhere
SMILES
Copy SMILES to clipboard
Cc1nnc(o1)c1ccc(nn1)N1CCC(CC1)Oc1cc(F)ccc1Cl
Background Reading
Miyazaki, M., Flowers, M.T., Sampath, H., et al. Hepatic stearoyl-CoA desaturase-1 deficiency protects mice from carbohydrate-induced adiposity and hepatic steatosis. Cell Metab6484-496(2007).
Dobrzyn, P., Sampath, H., Dobrzyn, A., et al. Loss of stearoyl-CoA desaturase 1 inhibits fatty acid oxidation and increases glucose utilization in the heart. Am J Physiol Endocrinol Metab294E357-E364(2008).
Cohen, P., Miyazaki, M., Socci, N.D., et al. Role for stearoyl-CoA desaturase-1 in leptin-mediated weight loss. Science297240-243(2002).
Liu, G., Lynch, J.K., Freeman, J., et al. Discovery of potent, selective, orally bioavailable stearoyl-CoA desaturase 1 inhibitors. J Med Chem503086-3100(2007).