| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
AZD-1656 (AZD 1656; AZD1656) is a novel and potent glucokinase (GK) activator with the potential for the treatment of T2DM (type 2 diabetes) and obesity.
| ln Vivo |
C57BL/6 mice treated with AZD1656 (0–9 mg/kg; oral gavage; daily; for 8 weeks) had lower blood glucose and glucose excursions and higher insulin levels. Numerous ChREBP target genes, such as G6pc, Pklr, Acly, Acac, and Gpd2, as well as carbohydrate response element binding protein beta isoform (ChREBP-β), can have their liver mRNA levels increased by AZD1656 [1].
|
|---|---|
| Animal Protocol |
Animal/Disease Models: C57BL/6 mice[1]
Doses: 0 mg/kg, 2 mg/kg, 4.5 mg/kg, 9 mg/kg Route of Administration: po (oral gavage); daily; 8 consecutive weeks Experimental Results: Oral glucose Take it 2 hrs (hrs (hours)) before a tolerance test to reduce blood sugar and glucose excursions and increase insulin levels. Male C57BL/6J0laHSD mice were used. For acute studies, food was withdrawn 4h before glucose gavage. Mice were gavaged with AZD1656 at doses of 2-9 mg/kg. Blood was sampled after 2h, followed by glucose gavage (2g/kg body wt) and further blood sampling. For chronic studies, mice received a powdered diet without or with AZD1656 added at doses to achieve 1 or 3 mg/kg body wt/day (based on a consumption of 4g diet/day). Treatment lasted for 4 or 8 weeks. Free-feeding blood samples were collected from the tail vein. For drug tolerance tests (DTT), mice were fasted for 2h, a blood sample was collected, followed by gavage with AZD1656 (dose equivalent to their daily dietary intake), and blood was sampled after 2h. At the end of the study, mice were culled for whole liver analysis or hepatocyte isolation. [1] |
| References |
|
| Additional Infomation |
AZD-1656 is being studied in the clinical trial NCT00747175 (a study evaluating the safety, tolerability, and P-Glucose of AZD1656 in patients with type 2 diabetes after multiple escalations of oral dose).
|
| Exact Mass |
478.196
|
|---|---|
| CAS # |
919783-22-5
|
| PubChem CID |
16039797
|
| Appearance |
White to off-white solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
635.0±55.0 °C at 760 mmHg
|
| Flash Point |
337.8±31.5 °C
|
| Vapour Pressure |
0.0±1.9 mmHg at 25°C
|
| Index of Refraction |
1.631
|
| LogP |
-0.21
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
35
|
| Complexity |
710
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
O=C(C1C=NC(=CN=1)OC1=CC(C(NC2C=NC(C)=CN=2)=O)=CC(=C1)O[C@@H](C)COC)N1CCC1
|
| InChi Key |
FJEJHJINOKKDCW-INIZCTEOSA-N
|
| InChi Code |
InChI=1S/C24H26N6O5/c1-15-10-27-21(12-25-15)29-23(31)17-7-18(34-16(2)14-33-3)9-19(8-17)35-22-13-26-20(11-28-22)24(32)30-5-4-6-30/h7-13,16H,4-6,14H2,1-3H3,(H,27,29,31)/t16-/m0/s1
|
| Chemical Name |
3-[5-(azetidine-1-carbonyl)pyrazin-2-yl]oxy-5-[(2S)-1-methoxypropan-2-yl]oxy-N-(5-methylpyrazin-2-yl)benzamide
|
| Synonyms |
AZD-1656 AZD 1656 AZD1656
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~522.47 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.35 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.35 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.35 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01221519 | COMPLETED | Drug: AZD1656 | High Blood Sugar Type 2 Diabetes Mellitus |
AstraZeneca | 2010-09 | Phase 1 |
| NCT00817505 | COMPLETED | Drug: AZD1656 Drug: AZD1656 |
Type 1 Diabetes | AstraZeneca | 2008-12 | Phase 1 |
| NCT01095991 | COMPLETED | Drug: AZD1656 Drug: Sitagliptin |
Type 2 Diabetes Mellitus | AstraZeneca | 2010-03 | Phase 1 |
| NCT01096940 | COMPLETED | Drug: AZD1656 Drug: simvastatin |
Type 2 Diabetes Mellitus | AstraZeneca | 2010-03 | Phase 1 |
| NCT01082120 | COMPLETED | Drug: AZD1656 Drug: Pioglitazone |
Type 2 Diabetes Mellitus | AstraZeneca | 2010-02 | Phase 1 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
