Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AMG-3969 is an effective glucokinase-glucokinase regulatory protein interaction (GK-GKRP) disruptor (IC50: 4 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 147.00 | |
5 mg | In stock | $ 347.00 | |
10 mg | In stock | $ 497.00 | |
25 mg | In stock | $ 793.00 | |
50 mg | In stock | $ 1,130.00 | |
100 mg | In stock | $ 1,520.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 397.00 |
Description | AMG-3969 is an effective glucokinase-glucokinase regulatory protein interaction (GK-GKRP) disruptor (IC50: 4 nM). |
Targets&IC50 | GK-GKRP:4 nM (cell free) |
In vitro | AMG-3969 exhibits potent cellular activity (EC50: 0.202 μM; IC50: 4 nM) [1,2]. AMG-3969 effectively reverses the inhibitory effect of GKRP on GK activity and promotes GK translocation in vitro (isolated hepatocytes) [3]. |
In vivo | AMG-3969, at a dosage of 100 mg/kg, significantly lowers blood glucose levels, achieving a 56% reduction eight hours post-administration [1]. This compound effectively normalizes blood glucose levels across various rodent diabetes models and exhibits favorable in vivo pharmacokinetic properties in rats (75%). It also progressively reduces blood glucose levels in db/db mice in a dose-responsive manner [2]. Demonstrating efficacy across three diabetes models—diet-induced obese (DIO), ob/ob, and db/db mice, AMG-3969, however, does not impact blood glucose in normoglycemic C57BL/6 (B6) mice. Additionally, it is highly efficient in enhancing carbohydrate metabolism, leading to noticeable prolonged effects on carbohydrate oxidation, evident from the increased respiratory exchange ratio observed up to the following day post a single administration [3]. |
Animal Research | Diabetic db/db mice are used in the study. At 8:00 AM, mice are bled via retro-orbital sinus puncture and blood glucose values are determined and used to randomize the animals in which their averages are similar, and only mice with blood glucose ranges between 300 and 500 mg/dL are included. Vehicle (2% hydroxypropyl methylcellulose, 1% Tween 80, pH 2.2 adjusted with MSA) or AMG-3969 (10, 30, 100 mg/kg) are gavaged at 9:00 AM. Blood glucose is measured at 4, 6, or 8 h posttreatment. At each time point, a 15 μL sample of whole blood is analyzed for drug exposure [1]. |
Molecular Weight | 522.46 |
Formula | C21H20F6N4O3S |
CAS No. | 1361224-53-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (191.40 mM)
You can also refer to dose conversion for different animals. More
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AMG-3969 1361224-53-4 Metabolism Glucokinase Hexokinase IV AMG3969 Hexokinase D AMG 3969 Inhibitor inhibit inhibitor