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A-769662
| Product Name | A-769662 |
| Price: | Inquiry |
| Catalog No.: | CN00353 |
| CAS No.: | 844499-71-4 |
| Molecular Formula: | C20H12N2O3S |
| Molecular Weight: | 360.39 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | N#Cc1c(=O)[nH]c2c(c1O)c(cs2)c1ccc(cc1)c1ccccc1O |
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| Description | A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM. |
| Target | AMPK:0.8 μM (EC50) |
| In Vitro | A-769662 is equally potent in activating the baculovirus expressed α1,β1,γ1 recombinant isoform of AMPK (EC50=0.7 μM). A-769662 and A-592107 activate 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 μM, 1.9 μM, or 1.1 μM, respectively[1]. A-769662 activates endogenous AMPK in LKB1-expressing (HEK293) and LKB1-deficient (CCL13) cells. A-769662 allosterically activates AMPK complexes containing γ1 harboring a substitution of arginine residue 298 to glycine (R298G). A-769662 inhibits dephosphorylation of Thr-172 in the mutant γ1-containing complexes to a similar degree as seen in the wild-type complexes[2]. A769662 (300 μM) has toxic effects on MEF cells. A769662 reversibly inhibits the proteasomal activity[3]. |
| In Vivo | A-769662 (30 mg/kg, i.p.) significantly reduced the respiratory exchange ratio (RER) in the SD rat. There are 33% and 58% reductions of malonyl CoA levels in livers of animals treated with 30 mg/kg A-769662 (0.905 nmol/g) or 500 mg/kg metformin (0.574 nmol/g), respectively. A-769662 (30 mg/kg, b.i.d.) significantly decreases fed plasma glucose (30%-40% reduction), while the lower doses (3 and 10 mg/kg) of A-769662 had no effect on the in diabetic ob/ob mice[1]. |
| Animal Admin | After acclimation ob/ob and lean mice are randomized to the various treatment groups by body weight and fed glucose levels (tail snip) at 8 AM. Baseline plasma insulin samples are also taken from a subset of the animals representing each treatment group (n=10 ob/ob and n=10 lean ob/+ littermates). Two separate ob/ob and lean littermate studies are completed: 1) an initial 5 day study, and 2) a 14 day study to examine efficacy and more completely characterize the body weight change observed in the 5 day study. Treatment groups for the 5 day study are as follows: ob/ob vehicle (0.2% hydroxypropyl methylcellulose [HPMC], i.p., b.i.d.), A-592107 (10 or 100 mg/kg, i.p., b.i.d.), A-769662 (3 or 30 mg/kg, i.p., b.i.d.), AICAR (375 mg/kg, s.c., b.i.d.), or metformin (450 mg/kg, p.o., q.d., with vehicle in PM), and lean littermates treated with vehicle (i.p., b.i.d.). Treatment groups for the 14 day ob/ob and lean littermate study are as follows: ob/ob vehicle (0.2% HPMC, i.p., b.i.d.), A-769662 (3, 10, or 30 mg/kg, i.p., b.i.d.), or metformin, and lean littermates treated with vehicle or 30 mg/kg of A-769662 (i.p., b.i.d.). |
| Density | 1.6±0.1 g/cm3 |
| Boiling Point | 630.1±55.0 °C at 760 mmHg |
| Flash Point | 334.9±31.5 °C |
| Exact Mass | 360.056854 |
| PSA | 125.35000 |
| LogP | 2.81 |
| Vapour Pressure | 0.0±1.9 mmHg at 25°C |
| Storage condition | Store at +4°C |