TGX-221 是一种p110β-特定的抑制剂，在无细胞试验中IC50为 5 nM，作用于p110β的选择性是作用于p110α的1000倍。

＞98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

TGX-221；TGX 221

White to yellow powder

DMSO : 18.2 mg/mL (50 mM)

p110β,p110δ

The activity of TGX-221 against different isoforms is measured in an in vitro PI3K assay using multiple preparations of recombinant p85/p110. TGX-221 show slow potent to p110δ with IC50 of 211 nM. Furthermore, TGX-221 partially attenuates insulin-induced phosphorylation of Ser473 of PKB in J774.2 macrophage cells. TGX-221 inhibits platelet-ECC interaction, platelet aggregation and platelet-granulocyte binding in an extracorporeal circulation (ECC) model. A recent study shows that after treatment with TGX-221 (0.2, 2, and 20 μM), PC3 cells show inhibition of proliferation with a significant reduction of the activity of the p110β PI3K isoform.

As an anti-thrombotic agent, TGX-221 at doses 1 + 1 (49 %) and 3+3 (88 %) improves integrated blood flow over 30 minutes in a mouse model. In addition, Tail bleeding time (BT) (sec) increases with TGX-221 doses of 3 + 3 (median 1560) and 1 + 1 (1305) and mean renal BT (sec) also increases in all TGX-221 groups.

[1] Chaussade C, et al. Biochem J. 2007, 404(3), 449-458.

[2] Straub A, et al. Thromb Haemost. 2008, 99(3), 609-615.

[3] Lu XY, et al. Appl Microbiol Biotechnol. 2011, 89(5), 1423-1433.

[4] Bird JE, et al. Thromb Res. 2011, 127(6), 560-564.

[5] Jackson SP, et al. Nat Med. 2005, 11(5), 507-514.