| Identification | Back Directory | [Name]
CAY10566 | [CAS]
944808-88-2 | [Synonyms]
CAY10566
2-(6-(4-(2-CHLORO-5-FLUOROPHENOXY)PIPERIDIN-1-YL)PYRIDAZIN-3-YL)-5-METHYL-1,3,4-OXADIAZOLE
3-[4-(2-CHLORO-5-FLUOROPHENOXY)-1-PIPERIDINYL]-6-(5-METHYL-1,3,4-OXADIAZOL-2-YL)-PYRIDAZINE
Pyridazine, 3-[4-(2-chloro-5-fluorophenoxy)-1-piperidinyl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)- | [Molecular Formula]
C18H17ClFN5O2 | [MDL Number]
MFCD11976899 | [MOL File]
944808-88-2.mol | [Molecular Weight]
389.81 |
| Chemical Properties | Back Directory | [Melting point ]
160 - 170°C | [Boiling point ]
600.2±65.0 °C(Predicted) | [density ]
1.369±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO (Slightly), Methanol (Slightly) | [form ]
Solid | [pka]
2.01±0.10(Predicted) | [color ]
Pale Beige |
| Hazard Information | Back Directory | [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. 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. 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 7.9 and 6.8 nM, respectively, when heptadecanoic acid and palmitic acid are used as the substrate. | [Uses]
CAY10566, is a stearoyl-CoA desaturase (SCD) inhibitor. | [in vivo]
After establishment of palpable tumors, the mice are treated with vehicle or SCD1 inhibitor (2.5 mg/kg CAY10566 orally twice daily). The effect of SCD1 inhibition on the Akt-driven tumors is greater than on the Ras-driven tumors, with the mean tumor volume at day 13 or 14 post therapy, relative to untreated tumors, 0.5±0.04 and 0.67±0.05 respectively (P=0.01 for Ras-Akt comparison, by two-tailed t test)[4]. | [storage]
Store at -20°C | [References]
[1] PAUL COHEN. Role for Stearoyl-CoA Desaturase-1 in Leptin-Mediated Weight Loss[J]. Science, 2002, 297 5579. DOI: 10.1126/science.1071527
[2] PAWEL DOBRZYN. Loss of stearoyl-CoA desaturase 1 inhibits fatty acid oxidation and increases glucose utilization in the heart.[J]. American journal of physiology. Endocrinology and metabolism, 2008: E357-64. DOI: 10.1152/ajpendo.00471.2007
[3] MAKOTO MIYAZAKI. Hepatic stearoyl-CoA desaturase-1 deficiency protects mice from carbohydrate-induced adiposity and hepatic steatosis.[J]. Cell metabolism, 2007, 6 6: 484-496. DOI: 10.1016/j.cmet.2007.10.014
[4] GANG LIU. Discovery of Potent, Selective, Orally Bioavailable Stearoyl-CoA Desaturase 1 Inhibitors[J]. Journal of Medicinal Chemistry, 2007, 50 13: 3086-3100. DOI: 10.1021/jm070219p
[5] BENJAMIN M VINCENT. Inhibiting Stearoyl-CoA Desaturase Ameliorates α-Synuclein Cytotoxicity.[J]. Cell reports, 2018: 2742-2754.e31. DOI: 10.1016/j.celrep.2018.11.028
[6] JUNMEI YI. Oncogenic activation of PI3K-AKT-mTOR signaling suppresses ferroptosis via SREBP-mediated lipogenesis.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2020: 31189-31197. DOI: 10.1073/pnas.2017152117
[7] LESLIE MAGTANONG . Exogenous Monounsaturated Fatty Acids Promote a Ferroptosis-Resistant Cell State[J]. Cell Chemical Biology, 2019, 26 3: Pages 420-432.e9. DOI: 10.1016/j.chembiol.2018.11.016 |
|
| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
|