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BPN-14136

Chemical Structure : BPN-14136

CAS No.: 1628945-93-6

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BPN-14136 (BPN14136)

Catalog No.: PC-20718Not For Human Use, Lab Use Only.

BPN-14136 is a potent, selective and non-retinoid RBP4 antagonist with SPA IC50 of 12.8 nM and HTRF IC50 of 43.6 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

BPN-14136 is a potent, selective and non-retinoid RBP4 antagonist with SPA IC50 of 12.8 nM and HTRF IC50 of 43.6 nM.
BPN-14136 does not induce human PXR activation, and displays no significant off-target activity at the hERG channel or within a standard screening panel of fifty-five GPCRs, enzymes, ion channels, and transporters.
BPN-14136 induces a robust and sustained lowering (>90%) of serum RBP4 levels upon 7-day QD oral dosing studies conducted in rats.

Physicochemical Properties

M.Wt 391.39
Formula C20H20F3N3O2
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

O=C(C1=NC(N2C[C@]3([H])[C@](C[C@H](C4=CC=CC=C4C(F)(F)F)C3)([H])C2)=NC(C)=C1)O

References

1. Boglarka Racz, et al. J Biol Chem. 2018 Jul 20;293(29):11574-11588.

2. Cioffi C. L et al. J. Med. Chem. 58, 5863–5888 10.1021/acs.jmedchem.5b00423

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