NS11394 是可口服GABAA的阳性变构调节剂 (PAM)，Ki值为 0.5 nM。它对GABAA的选择性依次为 α5、α3、α2 和α1 受体，具有抗炎和抗焦虑活性。

NS11394 is a effective and subtype-selective GABA(A) receptor-positive modulator; possesses a functional efficacy selectivity profile of α(5) >α(3) >α(2) >α(1) at GABA(A) alpha subunit-containing receptors.

Inhibition of FLT3 autophosphorylation: To measure inhibition of FLT3 autophosphorylation, MV4-11 or RS4;11 cells are cultured in low serum media (0.5% FBS) overnight and seeded at a density of 400 000 cells per well in a 96-well plate the following day. The cells are incubated with different concentrations of AC220 for 2 hours at 37 °C. To induce FLT3 autophosphorylation in RS4;11 cells, 100 ng/mL FLT3 ligand is added for 15 minutes after the 2-hour AC220 incubation. Cell lysates are prepared and incubated in 96-well plates precoated with a total FLT3 capture antibody. The coated plates are incubated with either a biotinylated antibody against FLT3 to detect total FLT3 or an antibody against phosphotyrosines to detect FLT3 autophosphorylation. In both cases, a SULFO-tagged streptavidin secondary antibody is used for electrochemiluminescence detection on the Meso Scale Discovery platform. The concentration of AC220 that inhibits FLT3-ITD or TLT3-WT autophosphorylation by 50% represents IC50 value

951650-22-9

C23H19N3O

353.425

NS 11394

DMSO:43 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years