A-769662 - Moligand™, 10mM in DMSO , CAS No.844499-71-4

CAS: 844499-71-4 Cat. No.: A407840 Molecular Weight: 360.39 EC Number: 878-650-7

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

Thieno[2,3-b]pyridine-5-carbonitrile, 6,7-dihydro-4-hydroxy-3-(2'-hydroxy[1,1'-biphenyl]-4-yl)-6-oxo-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

A-769662 A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM in cell-free assays, little effect on GPPase/FBPase activity.
In vitro

A-769662 stimulates partially purified rat liver AMPK with EC50 with 0.8 μM. A-769662 activates AMPK purified from multiple tissues and species in a dose-responsive manner with modest variations in observed EC50s. EC50s determined for A-769662 using partially purified AMPK extracts from rat heart, rat muscle, or human embryonic kidney cells (HEKs) are 2.2 mM, 1.9 mM, or 1.1 mM, respectively. A 4 hours treatment of primary rat hepatocytes with A-769662 dose-dependently increases ACC phosphorylation, which correlated inhibition of fatty acid synthesis with IC50 of 3.2 μM. A-769662 also inhibits fatty acid sythesis in mouse hepatocytes with IC50 with 3.6 μM A-769662 activates AMPK both allosterically and by inhibiting dephosphorylation of AMPK on Thr-172, similar to the effects of AMP. A-769662 inhibits proteasomal function by an AMPK-independent mechanism. A-769662 affects the in vitro activity of purified 26S proteasomes but not the in vitro activity of purified 20S proteasomes. A-769662 has toxic effects on MEF cells. A recent research shows A-769662 inhibited cell proliferation and DNA synthesis.

In vivo

Short-term treatment of normal Sprague Dawley rats with A-769662 decreases liver malonyl CoA levels and the respiratory exchange ratio, VCO2/VO2, indicating an increased rate of whole-body fatty acid oxidation. Treatment of ob/ob mice with 30 mg/kg b.i.d. A-769662 decreases hepatic expression of PEPCK, G6Pase, and FAS, lowers plasma glucose by 40%, reduced body weight gain and significantly decreases both plasma and liver triglyceride levels.
Cell Data

cell lines：

Concentrations：300 μM

Incubation Time：24 hours

Powder Purity:≥98%

Specifications

Synonyms

Thieno[2, 3-b]pyridine-5-carbonitrile, 6, 7-dihydro-4-hydroxy-3-(2'-hydroxy[1, 1'-biphenyl]-4-yl)-6-oxo-

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM in cell-free assays, little effect on GPPase/FBPase activity.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

ACTIVATOR

Names and Identifiers

• Isomeric SMILES: C1=CC=C(C(=C1)C2=CC=C(C=C2)C3=CSC4=C3C(=C(C(=O)N4)C#N)O)O
• Molecular Weight: 360.39
• Reaxy-Rn: 12162992
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12162992&ln=

Chemical and Physical Properties

• Refractive Index: 1.78
• Boil Point(°C): 630.08° C at 760 mmHg
• Melt Point(°C): 268.39°C