RBP4 antagonist 59

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Chemical Structure : RBP4 antagonist 59

Catalog No.: PC-20717Not For Human Use, Lab Use Only.

RBP4 antagonist 59 is a potent, selective and orally bioavailable retinol-binding protein 4 (RBP4) antagonist with HTRF IC50 of 16 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

RBP4 antagonist 59 is a potent, selective and orally bioavailable retinol-binding protein 4 (RBP4) antagonist with HTRF IC50 of 16 nM.
RBP4 antagonist 59 does not display any off-target pharmacology at KOR or at any other target within a screening panel.
RBP4 antagonist 59 (20 mg/kg per day) reduces circulating levels of adipose-derived RBP4 in the mouse transgenic model of hepatic steatosis.
RBP4 antagonist 59 partially prevents high-fat diet-induced obesity in adi-hRBP4 mice, reduces hepatic free fatty acid and triglyceride levels in obese adi-hRBP4 mice.

Physicochemical Properties

M.Wt	417.37
Formula	C20H15F4N5O
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
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Solubility	10 mM in DMSO
Chemical Name/SMILES	N#CC1=CN2C(C=C1)=NN=C2C(N3CCC(C4=CC=CC(F)=C4C(F)(F)F)CC3)=O

References

1. Christopher L Cioffi, et al. J Med Chem. 2019 Jun 13;62(11):5470-5500.

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