[CAS NO. 919783-22-5] AZD1656
PRODUCTS SPECIFICATIONS [919783-22-5]
DESCRIPTION [919783-22-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 478.50 |
| Molecular Formula | C24H26N6O5 |
| SMILES | O=C(NC1=NC=C(C)N=C1)C2=CC(O[C@@H](C)COC)=CC(OC3=NC=C(C(N4CCC4)=O)N=C3)=C2 |
Summary
AZD1656 is a potent, selective and orally active glucokinase activator with an EC 50 of 60 nM. AZD1656 has the potential for type 2 diabetes research [1] [2] [3] .
IC50 & Target
EC50: 60 nM (Glucokinase) [2]
In Vivo
AZD1656 (0-9 mg/kg; oral gavage; daily; for 8 weeks; C57BL/6 mice) treatment shows lowered blood glucose and glucose excursion and raised insulin. Liver mRNA levels for various ChREBP target genes including carbohydrate response element binding protein beta isoform (ChREBP-β), G6pc, Pklr, Acly, Acac and Gpd2 are increased by AZD1656 [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | C57BL/6 mice [1] |
| Dosage: | 0 mg/kg, 2 mg/kg, 4.5 mg/kg, 9 mg/kg |
| Administration: | Oral gavage; daily; for 8 weeks |
| Result: | Administered 2 hours before the oral glucose tolerance test, lowered blood glucose and glucose excursion and raised insulin. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01095991 | AstraZeneca |
Type 2 Diabetes Mellitus
|
March 2010 | Phase 1 |
| NCT01221545 | AstraZeneca |
Type 2 Diabetes Mellitus
|
October 2010 | Phase 1 |
| NCT00726427 | AstraZeneca |
Healthy
|
July 2008 | Phase 1 |
| NCT00960791 | AstraZeneca |
Type II Diabetes Mellitus
|
July 2009 | Phase 1 |
| NCT00741689 | AstraZeneca |
Healthy Volunteers
|
August 2008 | Phase 1 |
| NCT01069926 | AstraZeneca |
Glucose Lowering
|
March 2010 | Phase 1 |
| NCT00817778 | AstraZeneca |
Type 2 Diabetes
|
January 2009 | Phase 2 |
| NCT00768105 | AstraZeneca |
Type 2 Diabetes
|
September 2008 | Phase 1 |
| NCT00774553 | AstraZeneca |
Type 2 Diabetes
|
October 2008 | Phase 1 |
| NCT01020123 | AstraZeneca |
Type II Diabetes Mellitus
|
October 2009 | Phase 2 |
| NCT01082120 | AstraZeneca |
Type 2 Diabetes Mellitus
|
February 2010 | Phase 1 |
| NCT00790153 | AstraZeneca |
Type 2 Diabetes
|
November 2008 | Phase 1 |
| NCT00916604 | AstraZeneca |
Type 2 Diabetes
|
May 2009 | Phase 1 |
| NCT01083212 | AstraZeneca |
Type 2 Diabetes Mellitus
|
March 2010 | Phase 1 |
| NCT01103622 | AstraZeneca |
Type 2 Diabetes Mellitus
|
June 2010 | Phase 1 |
| NCT01103609 | AstraZeneca |
Type 2 Diabetes Mellitus
|
April 2010 | Phase 1 |
| NCT05216172 | Queen Mary University of London|AstraZeneca |
Type 2 Diabetes|Diabetes Mellitus, Type 2|Renal Transplant|Kidney Transplant; Complications|End Stage Renal Disease
|
January 21, 2020 | Phase 2 |
| NCT00856908 | AstraZeneca |
Type II Diabetes
|
February 2009 | Phase 2 |
| NCT00817271 | AstraZeneca |
Type 2 Diabetes
|
February 2009 | Phase 1 |
| NCT00747175 | AstraZeneca |
Type 2 Diabetes
|
August 2008 | Phase 1 |
| NCT01221519 | AstraZeneca |
Type 2 Diabetes Mellitus|High Blood Sugar
|
September 2010 | Phase 1 |
| NCT00995787 | AstraZeneca |
Type II Diabetes Mellitus
|
October 2009 | Phase 1 |
| NCT01096940 | AstraZeneca |
Type 2 Diabetes Mellitus
|
March 2010 | Phase 1 |
| NCT00819884 | AstraZeneca |
Type II Diabetes
|
January 2009 | Phase 1 |
| NCT01152385 | AstraZeneca |
Type 2 Diabetes Mellitus
|
May 2010 | Phase 2 |
| NCT00817505 | AstraZeneca |
Type 1 Diabetes
|
December 2008 | Phase 1 |
| NCT04516759 | St George Street Capital |
Covid19
|
August 12, 2020 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 250 mg/mL ( 522.47 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.0899 mL | 10.4493 mL | 20.8986 mL |
| 5 mM | 0.4180 mL | 2.0899 mL | 4.1797 mL |
| 10 mM | 0.2090 mL | 1.0449 mL | 2.0899 mL |
References
- [1] Brian E Ford, et al. Chronic glucokinase activator treatment activates liver Carbohydrate response element binding protein and improves hepatocyte ATP homeostasis during substrate challenge. Diabetes Obes Metab. 2020 Jun 10.
- [2] Medicinal Chemistry, et al. Design and Development of the Glucokinase Activator AZD1656. Complete Accounts of Integrated Drug Discovery and Development: Recent Examples from the Pharmaceutical Industry Volume 1, 185-220.
- [3] Terri Mitchard, et al. The novel use of a heterozygous knockout mouse for embryofetal development assessment of a glucokinase activator. Birth Defects Res B Dev Reprod Toxicol. 2014 Apr;101(2):152-61.
