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ARRY-403

Name: ARRY-403
Brand: TargetMol
SKU: T30142
Price: 415 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T30142Cas No. 1138669-65-4

Alias ARRY-403, ARRY403, ARRY 403, AMG-151, AMG151, AMG 151

ARRY-403 is a novel glucokinase activator that reduces fasting and postprandial blood glucose in patients with type 2 diabetes.

ARRY-403

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Purity: 97.08%

Catalog No. T30142Alias ARRY-403, ARRY403, ARRY 403, AMG-151, AMG151, AMG 151Cas No. 1138669-65-4

ARRY-403 is a novel glucokinase activator that reduces fasting and postprandial blood glucose in patients with type 2 diabetes.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$415	In Stock	In Stock
5 mg	$826	In Stock	In Stock
10 mg	$1,120	In Stock	In Stock
25 mg	$1,650	In Stock	In Stock

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

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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:97.08%

ee:100%

Appearance:Solid

Color:White

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Product Introduction

Bioactivity

Description	ARRY-403 is a novel glucokinase activator that reduces fasting and postprandial blood glucose in patients with type 2 diabetes.
In vivo	Phase I studies have shown that ARRY-403 (AMG 151) activates glucokinase, a key enzyme in glucose homeostasis. The present randomized, placebo-controlled phase IIa study evaluated the dose-effect relationship of the glucokinase activator AMG 151 relative to placebo on fasting plasma glucose (FPG) in 236 patients (33-35 patients per arm) with type 2 diabetes treated with metformin. Patients received oral AMG 151 at 50, 100, or 200 mg twice daily, AMG 151 at 100, 200, or 400 mg once daily, or matching placebo for 28 days. A significant linear dose-effect trend was observed with the twice-daily regimen (p = 0.004) for change in FPG to day 28. No trend was observed with the once-daily regimen. A higher incidence of hypoglycemia and hypertriglyceridemia was observed with AMG 151 administration. AMG 151 significantly reduced FPG when administered twice daily but not when administered once daily in patients with type 2 diabetes treated with metformin.[1]
Synonyms	ARRY-403, ARRY403, ARRY 403, AMG-151, AMG151, AMG 151

Chemical Properties

Molecular Weight	454.52
Formula	C₂₀H₁₈N₆O₃S₂
Cas No.	1138669-65-4
Smiles	Cc1ncccc1Oc1cc(Sc2ccccn2)cnc1Nc1nc(ns1)[C@H](O)CO
Relative Density.	1.54 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: 50 mg/mL (110.01 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2001 mL	11.0006 mL	22.0012 mL	110.0062 mL
5 mM	0.4400 mL	2.2001 mL	4.4002 mL	22.0012 mL
10 mM	0.2200 mL	1.1001 mL	2.2001 mL	11.0006 mL
20 mM	0.1100 mL	0.5500 mL	1.1001 mL	5.5003 mL
50 mM	0.0440 mL	0.2200 mL	0.4400 mL	2.2001 mL
100 mM	0.0220 mL	0.1100 mL	0.2200 mL	1.1001 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