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CAY10566

Cat. No. M9937
CAY10566 Structure
Synonym:

CAY-10566

Size Price Availability Quantity
5mg USD 197  USD197 In stock
10mg USD 297  USD297 In stock
25mg USD 587  USD587 In stock
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Quality Control & Documentation
Biological Activity

CAY10566 is a potent and selective inhibitor of SCD1 (stearoyl-CoA desaturase1) that demonstrates IC50 values of 4.5 and 26 nM in mouse and human enzymatic assays, respectively. CAY10566 treatment decreases Swiss 3T3 cell proliferation with concentration of 0.0001-10 μM. CAY10566 (2.5 mg/kg; orally twice daily) has great effect on mice with tumors.

Chemical Information
Molecular Weight 389.81
Formula C18H17ClFN5O2
CAS Number 944808-88-2
Solubility (25°C) DMSO 20 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Shabnam Fayezi, et al. Reprod Sci. Primary Culture of Human Cumulus Cells Requires Stearoyl-Coenzyme A Desaturase 1 Activity for Steroidogenesis and Enhancing Oocyte In Vitro Maturation

[2] Jurre J Kamphorst, et al. Proc Natl Acad Sci U S A. Hypoxic and Ras-transformed cells support growth by scavenging unsaturated fatty acids from lysophospholipids

[3] Andreas Koeberle, et al. J Biol Chem. Palmitoleate is a mitogen, formed upon stimulation with growth factors, and converted to palmitoleoyl-phosphatidylinositol

[4] Masashi Masuda, et al. J Lipid Res. Activating transcription factor 4 regulates stearate-induced vascular calcification

[5] Gang Liu, et al. J Med Chem. Discovery of potent, selective, orally bioavailable stearoyl-CoA desaturase 1 inhibitors

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Keywords: CAY10566, CAY-10566 supplier, inhibitors, activators


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