EX229 是一个苯并咪唑的衍生物，是 AMP 活化蛋白激酶 (AMPK) 的有效变构激动剂，其对 α1β1γ1、α2β1γ1 和 α1β2γ1 的 K_d 值分别为 0.06 μM、0.06 μM 和 0.51 μM。

EX229, a Benzimidazole derivative, is a potent and allosteric activator of AMP-activated protein kinase (AMPK), with K d s of 0.06 μM, 0.06 μM and 0.51 μM for α1β1γ1, α2β1γ1 and α1β2γ1 in biolayer interferometry, respectively.

Solid

AMPK α1β1γ1 0.06 μM (Kd) AMPK α2β1γ1 0.06 μM (Kd)p

EX229 is a potent and allosteric activator of AMP-activated protein kinase (AMPK), with Kds of 0.06 μM, 0.06 μM and 0.51 μM for α1β1γ1, α2β1γ1 and α1β2γ1, respectively.. Treatment of hepatocytes with EX229 (991) alone results in a slight increase in the phosphorylation of AMPK and RAPTOR only at 0.3 μM, whereas a robust increase in ACC phosphorylation is readily observed and saturated at a concentration of 0.03 μM EX229. AICAR or C13 alone robustly increases T172 phosphorylation of AMPKα, and when 991 is coincubated, there is a modest additional dose-dependent increase in AMPKα phosphorylation. RAPTOR phosphorylation is modestly increased by AICAR or C13 alone, and it is dose dependently increased when coincubations are carried out with EX229. EX229 also dose dependently (0.01 and 0.1 μM) inhibits lipogenesis (34% and 63%, respectively), which is further reduced whe

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Xiao B, et al. Structural basis of AMPK regulation by small molecule activators. Nat Commun. 2013;4:3017.
[2]. Bultot L, et al. Benzimidazole derivative small-molecule 991 enhances AMPK activity and glucose uptake induced by AICAR or contraction in skeletal muscle. Am J Physiol Endocrinol Metab. 2016 Oct 1;311(4):E706-E719.

In Vitro: DMSO : 13 mg/mL (30.10 mM; Need ultrasonic and warming)配制储备液