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EX-229

  Cat. No.:  DC11634   Featured
Chemical Structure
1219739-36-2
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More than 5000 active chemicals with high quality for research!
Field of application
EX229 is a small molecule AMPK activator that dose-dependently increases AMPK activity of α1-, α2-, β1- and β2-containing complexes at 50 uM
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1219739-36-2
Chemical Name: 5-[[6-Chloranyl-5-(1-Methylindol-5-Yl)-1h-Benzimidazol-2-Yl]oxy]-2-Methyl-Benzoic Acid
Synonyms: Ex229;5-[[6-Chloranyl-5-(1-Methylindol-5-Yl)-1h-Benzimidazol-2-Yl]oxy]-2-Methyl-Benzoic Acid;4cfe;BDBM50195475;SB19033;5-[6-chloro-5-(1-methylindol-5-yl)-1h-benzimidazol-2-yl]oxy-2-methyl-benzoic acid;5-{[6-chloro-5-(1-methyl-1h-indol-5-yl)-1h-benzimidazol-2-yl]oxy}-2-methylbenzoic acid;5-{[6-chloro-5-(1-methyl-1H-indol-5-yl)-1H-1,3-benzodiazol-2-yl]oxy}-2-methylbenzoic acid
SMILES: ClC1=C([H])C2=C(C([H])=C1C1C([H])=C([H])C3=C(C([H])=C([H])N3C([H])([H])[H])C=1[H])N=C(N2[H])OC1C([H])=C([H])C(C([H])([H])[H])=C(C(=O)O[H])C=1[H]
Formula: C24H18ClN3O3
M.Wt: 431.8710
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: EX229, a Benzimidazole derivative, 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 in biolayer interferometry, respectively.
In Vitro: 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.[1]. 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 when it is coincubated with a low dose of AICAR (0.03 mM) or C13 (1 μM). Treatment with EX229 promotes dose-dependent increases in ACC and RAPTOR phosphorylation. Similar to the observations in hepatocytes[2].
References: [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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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