3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenol Chemical Properties

Boiling point:

699.6±65.0 °C(Predicted)

Density 

1.516±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

insoluble in H2O; insoluble in EtOH; ≥3.46 mg/mL in DMSO

form 

Yellow powder solid.

pka

8.54±0.10(Predicted)

3,3'-(2,4-Diamino-6,7-pteridinediyl)bisphenol Usage And Synthesis

Uses

TG100-115 is a potent and selective phosphoinositide 3-kinase gamma/delta (PI3Kγ/δ) inhibitor. It can provide potent cardioprotection, reduce infarct development, and preserve myocardial function.

Definition

ChEBI: 3-[2,4-diamino-7-(3-hydroxyphenyl)-6-pteridinyl]phenol is a member of pteridines.

Biological Activity

tg100-115 is an inhibitor of pi3kγ and pi3kδ with ic50 values of 83 nm and 235 nm, respectively. tg100-115 shows no obvious activity against pi3kα and pi3kβ [1].tg100-115 remarkably reduced eosinophil accumulation, balf levels of classic th2 cytokine il-13, perivascular and peribronchial leukocyte accumulations, and bronchiolar mucin accumulation in a murine model. besides, tg100-115 showed to reduce airway hyper-responsiveness (ahr) by approximately 50% in asthmatic mice. moreover, tg100-115 has been reported to reduce both smoke-and lps-induced neutrophil and lps-induced classic th1 cytokine tnfα accumulations in mice [2].

target

PI3K-γ

References

[1] doukas j1, wrasidlo w, noronha g, dneprovskaia e, fine r, weis s, hood j, demaria a, soll r, cheresh d. hosphoinositide 3-kinase gamma/delta inhibition limits infarct size after myocardial ischemia/reperfusion injury. proc natl acad sci u s a. 2006 dec 26;103(52):19866-71.
[2] doukas j1, eide l, stebbins k, racanelli-layton a, dellamary l, martin m, dneprovskaia e, noronha g, soll r, wrasidlo w, acevedo lm, cheresh da. aerosolized phosphoinositide 3-kinase gamma/delta inhibitor tg100-115 [3-[2,4-diamino-6-(3-hydroxyphenyl)pteridin-7-yl]phenol] as a therapeutic candidate for asthma and chronic obstructive pulmonary disease. j pharmacol exp ther. 2009 mar;328(3):758-65.

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