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3-[4-(2-chloro-5-fluorophenoxy)-1-piperidinyl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)-pyridazine (CAS 944808-88-2)

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Application:Buy CAS# 944808-88-2, a potent and selective inhibitor of SCD1
CAS Number:944808-88-2
Purity:≥98%
Molecular Weight:389.8
Molecular Formula:C18H17ClFN5O2
Refer to Certificate of Analysis for lot specific data (including water content).
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Product NameCatalog #UnitPriceQtyAddFavorites
3-[4-(2-chloro-5-fluorophenoxy)-1-piperidinyl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)-pyridazine sc-205109 1 mg $108
3-[4-(2-chloro-5-fluorophenoxy)-1-piperidinyl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)-pyridazine sc-205109A 5 mg $487
Description
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. Thus, modulating SCD1 activity pharmacologically may be a useful tool for regulating type 2 diabetes, dyslipidemia, and obesity. A potent and selective inhibitor of SCD1 that demonstrates IC50 values of 26 and 4.5 nM in human and murine enzymatic assays, respectively. This compound inhibits the conversion of saturated, long-chain fatty acyl-CoAs to monounsaturated, long-chain fatty acyl-CoAs in HepG2 cells with IC50 values of 6.8 and 7.9 nM, respectively when palmitic acid and heptadecanoic acid are used as the substrate.
Technical Information
Physical State:Solid
Solubility:Soluble in 1:5 DMF:PBS (pH 7.2) (~0.15 mg/mL), ethanol (~0.15 mg/mL), DMSO (~10 mg/mL), and DMF (~10 mg/mL).
Storage:Store at -20° C
IC50:SCD1 : IC50 = 4.5 nM (mouse); SCD1 : IC50 = 26 nM (human); the conversion of saturated, long-chain fatty acyl-CoAs to monounsaturated, long-chain fatty acyl-CoAs: IC50 = 7.9 nM (Hep-G2 cells); the conversion of saturated, long-chain fatty acyl-CoAs to monounsaturated, long-chain fatty acyl-CoAs: IC50 = 6.8 nM (Hep-G2 cells)
Safety and Reference Information
PubChem CID:16732433
SMILES:Cc1nnc(o1)c1ccc(nn1)N1CCC(CC1)Oc1cc(F)ccc1Cl
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
References
1 Cohen, P., Miyazaki, M., Socci, N.D., et al. Role for stearoyl-CoA desaturase-1 in leptin-mediated weight loss. Science 297 240-243 (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 Metab 294, E357-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 Metabolism 6 484-496 (2007). 4 Liu, G., Lynch, J.K., Freeman, J., et al. Discovery of potent, selective, orally bioavailable stearoyl-CoA desaturase 1 inhibitors. J Med Chem 50 3086-3100 (2007).
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