EX229 

Cat. No.: HY-112769 Purity: 98.37%
Handling Instructions

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.

For research use only. We do not sell to patients.

EX229 Chemical Structure

EX229 Chemical Structure

CAS No. : 1219739-36-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 187 In-stock
Estimated Time of Arrival: December 31
5 mg USD 170 In-stock
Estimated Time of Arrival: December 31
10 mg USD 270 In-stock
Estimated Time of Arrival: December 31
25 mg USD 560 In-stock
Estimated Time of Arrival: December 31
50 mg USD 960 In-stock
Estimated Time of Arrival: December 31
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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.

IC50 & Target

Kd: 0.06 μM (α1β1γ1), 0.06 μM (α2β1γ1), 0.51 μM (α1β2γ1)[1].

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].

Solvent & Solubility
In Vitro: 

DMSO : 5.4 mg/mL (12.50 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3155 mL 11.5776 mL 23.1551 mL
5 mM 0.4631 mL 2.3155 mL 4.6310 mL
10 mM 0.2316 mL 1.1578 mL 2.3155 mL
*Please refer to the solubility information to select the appropriate solvent.
Molecular Weight

431.87

Formula

C₂₄H₁₈ClN₃O₃

CAS No.

1219739-36-2

SMILES

O=C(O)C1=CC(OC2=NC3=CC(Cl)=C(C4=CC5=C(N(C)C=C5)C=C4)C=C3N2)=CC=C1C

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 98.37%

  • Am J Physiol Endocrinol Metab. 2016 Oct 1;311(4):E706-E719.杨火祥要求上线20181212;竞价
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Product Name:
EX229
Cat. No.:
HY-112769
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EX229

Cat. No.: HY-112769