Product Details
| Product Name:
AMG-3969 |
CAS No.:
1361224-53-4 |
| Purity:
99.65% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| Name | AMG-3969 |
| Description | AMG-3969 is an effective glucokinase-glucokinase regulatory protein interaction (GK-GKRP) disruptor (IC50: 4 nM). |
| 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]. |
| In vitro | AMG-3969 demonstrates significant cellular activity (EC50: 0.202 μM; IC50: 4 nM) [1,2], reversing GKRP's inhibitory effect on GK activity and promoting 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]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 100 mg/mL (191.40 mM)
|
| Keywords | Inhibitor | inhibit | Hexokinase IV | Hexokinase D | Glucokinase | AMG-3969 | AMG3969 | AMG 3969 |
| Inhibitors Related | ARRY-403 | Globalagliatin | ML251 | PFK-015 | 3PO | PFKFB3-IN-2 | Oxfendazole | AZ PFKFB3 26 | AMG-1694 | PFK-158 | Dorzagliatin | PF-04937319 |
| Related Compound Libraries | Glycometabolism Compound Library | Glycolysis Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Cancer Metabolism Compound Library | PPI Inhibitor Library | Metabolism Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Fluorochemical Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$38.00/1mg |
VIP5Y
|
TargetMol Chemicals Inc.
|
2024-11-19 |
|
|
$0.00/25KG |
VIP5Y
|
Hebei Mojin Biotechnology Co., Ltd
|
2024-10-10 |
United States