A-769662
Catalog No.: GC11234Purity:>98.50%Synonyms: A-769662;A769662
Ein direkter Aktivator von AMPK
Die Produkte sind ausschließlich für Forschungszwecke bestimmt. Nicht zur Anwendung am Menschen. Wir verkaufen nicht an Patienten.
Cas No.: 844499-71-4
10mM (in 1mL DMSO)In Stock
$53.00
1
10mgIn Stock
$49.00
1
25mgIn Stock
$106.00
1
50mgIn Stock
$191.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $53.00 | In Stock | 1 | |
| 10mg | $49.00 | In Stock | 1 | |
| 25mg | $106.00 | In Stock | 1 | |
| 50mg | $191.00 | In Stock | 1 |
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Zitate (Citations)
1 publicationsPublikationen von Forschern, die dieses Produkt verwendenBeschreibung (Description)
A-769662 is an activator of AMP-activated protein kinase[1], which has an EC50 value of 0.8μM[2]. A-769662 activated the activity of AMPK extracted from human embryonic kidney cells (HEKs) , rat muscle, or rat heart with EC50 values of 1.1mM , 1.9mM , or 2.2mM, respectively[3].
A-769662 ( 100μM , 36h ) activates AMPK signaling and tumor suppressor tuberous sclerosis complex 2 ( TSC2 ) phosphorylation[4]. A-769662 ( 100μM , 24h ) increased AMPK phosphorylation in normal rat kidney cells under normal glucose ( 5mM )[5].
A-769662 (400mg/mouse; 14 days; intraperitoneal injection) treatment reduced mouse colon tumor (CT26 mice tumor models) growth and resulted in long-term survivors[6]. A-769662 (20pmol, 3 days, intravitreal injection) protect mice from Methylglyoxal (MGO)-induced retinopathy[7].
A-769662 promoting AMPK activation can induce the autophagy through facilitation of autophagosome formation[8] .
References:
[1] GORANSSON O, MCBRIDE A, HAWLEY S A, et al. Mechanism of action of A-769662, a valuable tool for activation of AMP-activated protein kinase [J]. J Biol Chem, 2007, 282(45): 32549-60.
[2] COOL B, ZINKER B, CHIOU W, et al. Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome [J]. Cell Metab, 2006, 3(6): 403-16.
[3] MORENO D, KNECHT E, VIOLLET B, et al. A769662, a novel activator of AMP-activated protein kinase, inhibits non-proteolytic components of the 26S proteasome by an AMPK-independent mechanism [J]. FEBS Lett, 2008, 582(17): 2650-4.
[4] KAKADIA J H, KHALID M U, HEINEMANN I U, et al. AMPK-mTORC1 pathway mediates hepatic IGFBP-1 phosphorylation in glucose deprivation: a potential molecular mechanism of hypoglycemia-induced impaired fetal growth [J]. J Mol Endocrinol, 2024, 72(3):
[5] SHRIKANTH C B, JAGANNATH S, CHILKUNDA N D. AMPK differentially alters sulphated glycosaminoglycans under normal and high glucose milieu in proximal tubular cells [J]. J Biochem, 2021, 169(1): 75-86.
[6] DAI X, BU X, GAO Y, et al. Energy status dictates PD-L1 protein abundance and anti-tumor immunity to enable checkpoint blockade [J]. Mol Cell, 2021, 81(11): 2317-31 e6.
[7] SEKAR P, HSIAO G, HSU S H, et al. Metformin inhibits methylglyoxal-induced retinal pigment epithelial cell death and retinopathy via AMPK-dependent mechanisms: Reversing mitochondrial dysfunction and upregulating glyoxalase 1 [J]. Redox Biol, 2023, 64(102786.
[8] YERRA V G, ARETI A, KUMAR A. Adenosine Monophosphate-Activated Protein Kinase Abates Hyperglycaemia-Induced Neuronal Injury in Experimental Models of Diabetic Neuropathy: Effects on Mitochondrial Biogenesis, Autophagy and Neuroinflammation [J]. Mol Neurobiol, 2017, 54(3): 2301-12.
Protokoll (Protocol)
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Cell experiment[1]: |
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Cell lines |
The neuro2a (N2A) cell line. |
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Preparation method |
The N2A cell line from National Centre for Cell Sciences were grown in minimum essential medium (MEM) (containing 5mM glucose) supplemented with 10 % fetal bovine serum (FBS) , glutamine (2mM) , streptomycin/ penicillin (1%) , at 37℃, in a humidified atmosphere of 95% air and 5% CO2. High glucose condition was created by adding 25mM glucose to medium.The cells were treated with 25μM or 50μM A769662 within 24h. |
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Reaction Conditions |
25μM or 50μM within 24h. |
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Applications |
A769662 treatment ameliorates neuroinflammation in high glucose-exposed N2A cells. |
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Animal experiment[2]: |
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Animal models |
BALB/cJ female mice |
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Preparation method |
Tumors were established by subcutaneously injecting 1×105 tumor cells in 100mL HBSS into the right flank of BALB/cJ female mice .Seven days after tumor cells were injected, animals were pooled and randomly divided into designated experimental groups with comparable average tumor size. A769662 treatments were conducted by intraperitoneal injection (400mg per mouse in 200mL 5% DMSO + 10% polyethylene glycol + 1% Tween 80 in PBS buffer) every day for two weeks. |
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Dosage form |
400mg/mouse ; 2 weeks ; intraperitoneal injection. |
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Applications |
A769662 treatment reduced tumor growth and resulted in long-term survivors. |
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References: [1] YERRA V G, ARETI A, KUMAR A. Adenosine Monophosphate-Activated Protein Kinase Abates Hyperglycaemia-Induced Neuronal Injury in Experimental Models of Diabetic Neuropathy: Effects on Mitochondrial Biogenesis, Autophagy and Neuroinflammation [J]. Mol Neurobiol, 2017, 54(3): 2301-12. [2] DAI X, BU X, GAO Y, et al. Energy status dictates PD-L1 protein abundance and anti-tumor immunity to enable checkpoint blockade [J]. Mol Cell, 2021, 81(11): 2317-31 e6. |
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Produktdokumente (Product Documents)
Purity:>98.50%Appearance:A solid
Chemische Eigenschaften (Chemical Properties)
CAS-Nr.
844499-71-4
Synonyme
A-769662;A769662
Chemischer Name
4-hydroxy-3-[4-(2-hydroxyphenyl)phenyl]-6-oxo-7H-thieno[2,3-b]pyridine-5-carbonitrile
SMILES
C1=CC=C(C(=C1)C2=CC=C(C=C2)C3=CSC4=C3C(=C(C(=O)N4)C#N)O)O
Summenformel
C20H12N2O3S
Molekulargewicht
360.39
Löslichkeit
≥ 18.0195 mg/mL in DMSO
Lagerung
Store at -20°C
Allgemeine Hinweise
Wählen Sie anhand der Löslichkeitsdaten des Produkts ein geeignetes Lösungsmittel. Aliquotieren Sie die Stammlösung nach der Herstellung, um wiederholte Gefrier-Auftau-Zyklen zu vermeiden.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Versandbedingungen
Evaluierungsmuster werden mit Kühlakkus versandt. Andere verfügbare Größen werden bei Raumtemperatur oder auf Anfrage mit Kühlakkus versandt.
Rechner (Calculators)Molarität / Verdünnung / Molekulargewicht / Einheitenumrechnung / In-vivo-Formulierung / Löslichkeit
g/mol
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