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T-3764518

Chemical Structure : T-3764518

CAS No.: 1809151-56-1

T-3764518 (T 3764518;T3764518)

Catalog No.: PC-60369Not For Human Use, Lab Use Only.

T-3764518 (T 3764518, T3764518) is a novel potent, orally active SCD1 inhibitor with binding IC50 of 4.7 nM for hSCD1.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

T-3764518 (T 3764518, T3764518) is a novel potent, orally active SCD1 inhibitor with binding IC50 of 4.7 nM for hSCD1; induces phosphorylation and activation of AMPK in HCT-116 cells, which led to blockade of downstream fatty acid synthesis and acceleration of autophagy; shows significant pharmacodynamic marker reduction (at 0.3mg/kg, bid) in HCT116 mouse xenograft model and tumor growth suppression (at 1mg/kg, bid) in 786-O mouse xenograft model; exhibits an excellent PK profile.

Physicochemical Properties

M.Wt 473.379
Formula C20H17F6N5O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(5-(6-(4-(Trifluoromethyl)-4-(4-(trifluoromethyl)phenyl) piperidin-1-yl)pyridazin-3-yl)-1,3,4-oxadiazol-2-yl)methanol

References

1. Imamura K, et al. Bioorg Med Chem. 2017 Jul 15;25(14):3768-3779.

2. Nishizawa S, et al. Eur J Pharmacol. 2017 Jul 15;807:21-31.

3. Ono A, et al. PLoS One. 2017 Jul 13;12(7):e0181243.

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