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AMG-3969

Name: AMG-3969
Brand: TargetMol
SKU: TQ0055
Price: 50 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. TQ0055Cas No. 1361224-53-4

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

AMG-3969

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Purity: 99.65%

Catalog No. TQ0055Cas No. 1361224-53-4

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

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$50	In Stock	In Stock
5 mg	$119	In Stock	In Stock
10 mg	$191	In Stock	In Stock
25 mg	$320	In Stock	In Stock
50 mg	$443	In Stock	In Stock
100 mg	$592	In Stock	In Stock
200 mg	$822	-	In Stock
1 mL x 10 mM (in DMSO)	$140	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.65%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

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 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].
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].

Chemical Properties

Molecular Weight	522.46
Formula	C₂₁H₂₀F₆N₄O₃S
Cas No.	1361224-53-4
Smiles	CC#C[C@H]1CN(CCN1c1ccc(cc1)C(O)(C(F)(F)F)C(F)(F)F)S(=O)(=O)c1ccc(N)nc1
Relative Density.	1.56 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 100 mg/mL (191.4 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (7.66 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9140 mL	9.5701 mL	19.1402 mL	95.7011 mL
5 mM	0.3828 mL	1.9140 mL	3.8280 mL	19.1402 mL
10 mM	0.1914 mL	0.9570 mL	1.9140 mL	9.5701 mL
20 mM	0.0957 mL	0.4785 mL	0.9570 mL	4.7851 mL
50 mM	0.0383 mL	0.1914 mL	0.3828 mL	1.9140 mL
100 mM	0.0191 mL	0.0957 mL	0.1914 mL	0.9570 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc