DBPR108 Chemical Properties

Boiling point:

557.9±50.0 °C(Predicted)

Density 

1.20±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO : ≥ 25 mg/mL (77.07 mM)

form 

Solid

pka

7.63±0.30(Predicted)

color 

White to off-white

DBPR108 Usage And Synthesis

Uses

DBPR108 is a potent, selective, and orally bioavailable dipeptide-derived inhibitor of DPP4 with IC50 of 15 nM; no inhibition on DDP8 and DPP9. IC50 value: 15 nM [1] Target: DPP4 inhibitor DBPR108 is an IC50=15 nM DPP IV inhibitor displays a more than 3000-fold selectivity over DPP8 DPP9, FAP and DPP-II. TThe in vivo effects of DBPR108, including inhibition of plasma DPP-IV activity and suppression of blood glucose elevation, were also demonstrated. DBPR108 is a potent, selective, long-acting and safe DPP-IV inhibitor as a potential treatment of type 2 diabetes mellitus.

References

[1] Yeh TK, et al. (2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV. Bioorg Med Chem Lett. 2010 Jun DOI:10.1016/j.bmcl.2010.04.124