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AMG-3969

Catalog No. TQ0055   CAS 1361224-53-4

AMG-3969 is an effective glucokinase-glucokinase regulatory protein interaction (GK-GKRP) disruptor (IC50: 4 nM).

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AMG-3969 Chemical Structure
AMG-3969, CAS 1361224-53-4
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
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Purity: 98.89%
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Biological Description
Chemical Properties
Storage & Solubility Information
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 (100 mg/kg) demonstrates significant reductions in blood glucose with robust efficacy (56% reduction) observed at the 8 h time point [1]. AMG-3969 normalized blood glucose levels in several rodent models of diabetes. AMG-3969 has good in vivo pharmacokinetic (PK) properties in rats (75%) and significantly lowers blood glucose levels in a dose-dependent manner db/db mice [2]. AMG-3969 demonstrates dose-dependent efficacy in three models of diabetes: diet-induced obese (DIO), ob/ob and db/db mice; however, AMG-3969 is ineffective in lowering blood glucose in normoglycaemic C57BL/6 (B6) mice. AMG-3969 is highly effective in promoting carbohydrate substrate. AMG-3969 exhibits extended changes to carbohydrate oxidation as observed by increased respiratory exchange ratio into the next night and day after a single dose [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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (191.40 mM)

TargetMolReferences and Literature

1. Nishimura N, et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N'-arylpiperazine series. J Med Chem. 2014 Apr 10;57(7):3094-116. 2. Lloyd DJ, et al. Antidiabetic effects of glucokinase regulatory protein small-molecule disruptors. Nature. 2013 Dec 19;504(7480):437-40. 3. St Jean DJ Jr, et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J Med Chem. 2014 Jan 23;57(2):325-38.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Metabolism Compound Library Bioactive Compound Library Covalent Inhibitor Library Kinase Inhibitor Library PPI Inhibitor Library Metabolism Compound Library Glycolysis Compound Library Bioactive Compounds Library Max Glycometabolism Compound Library

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Keywords

AMG-3969 1361224-53-4 Metabolism Glucokinase Hexokinase IV AMG3969 Hexokinase D AMG 3969 Inhibitor inhibit inhibitor

 

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