PVM/MA Chemical Properties

Boiling point:

467.5±55.0 °C(Predicted)

Density 

1.491±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMF: 30 mg/ml; DMSO: 30 mg/ml; DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml

form 

A crystalline solid

pka

1.49±0.41(Predicted)

color 

Light yellow to light brown

InChI

InChI=1S/C14H13ClF6N6/c1-6(13(16,17)18)22-11-25-10(8-4-3-5-9(15)24-8)26-12(27-11)23-7(2)14(19,20)21/h3-7H,1-2H3,(H2,22,23,25,26,27)/t6-,7-/m1/s1

InChIKey

QCZAWDGAVJMPTA-RNFRBKRXSA-N

SMILES

N1=C(C2=NC(Cl)=CC=C2)N=C(N[C@H](C)C(F)(F)F)N=C1N[C@H](C)C(F)(F)F

PVM/MA Usage And Synthesis

Uses

PF-06291874 is a novel and potent glucagon receptor antagonist for the potential treatment of diabetes mellitus. PF-06291874, has a lower molcular weight and lipophilicity than historical glucagon receptor antagonists, resulting in excellent selectivity in broad-panel screening, lower cytotoxicity, and excellent overall in vivo safety in early pre-clinical testing.

Synthesis

Maleic anhydride (MA) was added to a solvent mixture of cyclohexane and ethyl acetate in a polymerizer equipped with an agitator, a reflux condenser, and an inner temperature-controlling device. The polymerizer was purged of air and filled with nitrogen. The solution was heated to 70 °C, and then an initiator solution (lauroyl peroxide dissolved in ethyl acetate) and Methyl vinyl ether (MVE) were added to the polymerizer in a dropwise manner. A slurry was obtained, which was filtered and dried under a vacuum to obtain a white powdery copolymer.

IC 50

IDH1; IDH2

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