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ARRY-403

Catalog No. T30142   CAS 1138669-65-4
Synonyms: AMG-151, ARRY 403, ARRY403, ARRY-403, AMG151, AMG 151

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

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ARRY-403 Chemical Structure
ARRY-403, CAS 1138669-65-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 988.00
5 mg In stock $ 1,980.00
10 mg In stock $ 2,670.00
25 mg In stock $ 3,960.00
50 mg In stock $ 5,330.00
100 mg In stock $ 7,190.00
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Purity: 98.69%
ee: 100%
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Biological Description
Chemical Properties
Storage & Solubility Information
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 AMG-151, ARRY 403, ARRY403, ARRY-403, AMG151, AMG 151
Molecular Weight 454.52
Formula C20H18N6O3S2
CAS No. 1138669-65-4

Storage

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

TargetMolReferences and Literature

1. Katz L, et al. AMG 151 (ARRY-403), a novel glucokinase activator, decreases fasting and postprandial glycaemia in patients with type 2 diabetes. Diabetes Obes Metab. 2016 Feb;18(2):191-5. 2. Chung J, et al. Utilizing physiologically based pharmacokinetic modeling to inform formulation and clinical development for a compound with pH-dependent solubility. J Pharm Sci. 2015 Apr;104(4):1522-32.

Related compound libraries

This product is contained In the following compound libraries:
Drug Repurposing Compound Library Bioactive Compounds Library Max Kinase Inhibitor Library Bioactive Compound Library

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Keywords

ARRY-403 1138669-65-4 Metabolism Glucokinase AMG-151 ARRY 403 ARRY403 AMG151 AMG 151 inhibitor inhibit

 

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