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CAY10566 shows excellent cellular activity in blocking the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells (IC50=7.9 nM or 6.8 nM). CAY10566 is a potent, orally bioavailable and selective stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50s of 4.5 and 26 nM in mouse and human enzymatic assays, respectively..
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | 44 € | In Stock | |
5 mg | 147 € | In Stock | |
10 mg | 227 € | In Stock | |
25 mg | 463 € | In Stock | |
50 mg | 680 € | In Stock | |
100 mg | 937 € | In Stock | |
500 mg | 1.871 € | In Stock | |
1 mL x 10 mM (in DMSO) | 126 € | In Stock |
Description | CAY10566 shows excellent cellular activity in blocking the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells (IC50=7.9 nM or 6.8 nM). CAY10566 is a potent, orally bioavailable and selective stearoyl |
Targets&IC50 | SCD1 (mouse):4.5 nM (IC50), SCD1 (human):26 nM (IC50) |
In vitro | CAY10566 (0.0001-10 μM; 24 hours) concentration-dependently decreases Swiss 3T3 cell proliferation [3]. |
In vivo | Upon the formation of detectable tumors, mice receive either a placebo or the SCD1 inhibitor CAY10566 (2.5 mg/kg orally twice daily). SCD1 inhibition demonstrates a more pronounced effect on Akt-driven tumors compared to Ras-driven tumors. Specifically, the average tumor volume on days 13 or 14 after treatment, compared to control tumors, was 0.5±0.04 for Akt-driven tumors and 0.67±0.05 for Ras-driven tumors (P=0.01 for Ras-Akt comparison, according to a two-tailed t-test) [4]. |
Molecular Weight | 389.81 |
Formula | C18H17ClFN5O2 |
Cas No. | 944808-88-2 |
Smiles | Cc1nnc(o1)-c1ccc(nn1)N1CCC(CC1)Oc1cc(F)ccc1Cl |
Relative Density. | 1.369 g/cm3 (Predicted) |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 24 mg/mL (61.57 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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