[CAS NO. 1191995-00-2] Dorzagliatin
PRODUCTS SPECIFICATIONS [1191995-00-2]
DESCRIPTION [1191995-00-2]
Overview
| MDL | MFCD22376579 |
|---|---|
| Molecular Weight | 462.93 |
| Molecular Formula | C22H27ClN4O5 |
| SMILES | O=C(NC1=NN(C[C@@H](O)CO)C=C1)[C@@H](N2CC(OC(C=CC=C3)=C3Cl)=CC2=O)CC(C)C |
Summary
Dorzagliatin (HMS5552), a dual-acting glucokinase (GK) activator, improves glycaemic control and pancreatic β-cell function in type 2 diabetes [1] .
IC50 & Target
Glucokinase [1]
In Vivo
Dorzagliatin (low-dose 10 mg/kg, and high-dose 30 mg/kg; administered intragastrically; daily 8:00 AM for one month) exerts a glucose-lowering effect on the glucose levels in diabetic rats [2 .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male Sprague-Dawley (SD) rats (aged approximately 6–8 weeks and weighing 200-230 g) [2 |
| Dosage: | Low-dose (10 mg/kg), and high-dose (30 mg/kg) |
| Administration: | Administered intragastrically (i.g.); daily (8:00 AM) for one month |
| Result: | Exerted a glucose-lowering effect on the glucose levels. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT04080596 | Hua Medicine Limited |
Drug Interaction
|
October 13, 2017 | Phase 1 |
| NCT04426708 | Hua Medicine Limited |
Type 2 Diabetes Mellitus
|
February 18, 2019 | Phase 1 |
| NCT03790839 | Hua Medicine Limited |
Patients
|
January 31, 2019 | Phase 1 |
| NCT05468229 | Chinese University of Hong Kong |
Glucose Intolerance
|
August 2022 | Phase 1|Phase 2 |
| NCT03173391 | Hua Medicine Limited|Tigermed Consulting Co., Ltd |
Diabetes Mellitus, Type 2
|
July 18, 2017 | Phase 3 |
| NCT03790787 | Hua Medicine Limited |
Patients
|
April 18, 2019 | Phase 1 |
| NCT04324424 | Hua Medicine Limited |
Type 2 Diabetes Mellitus
|
April 23, 2019 | Phase 1 |
| NCT02077452 | Hua Medicine Limited |
Type 2 Diabetes Mellitus
|
March 2014 | Phase 1 |
| NCT04531631 | Chinese University of Hong Kong |
Diabetes Mellitus, Type 2
|
September 30, 2020 | Phase 2 |
| NCT02597400 | Hua Medicine Limited |
Type 2 Diabetes Mellitus
|
October 2015 | Phase 1 |
| NCT03141073 | Hua Medicine Limited|Covance |
Diabetes Mellitus, Type 2
|
October 15, 2017 | Phase 3 |
| NCT02386982 | Hua Medicine Limited |
Type 2 Diabetes
|
March 2015 | Phase 1 |
| NCT05098470 | University of Virginia |
Type 2 Diabetes
|
March 7, 2022 | Phase 3 |
| NCT04080609 | Hua Medicine Limited |
Drug Interaction
|
March 27, 2018 | Phase 1 |
| NCT02561338 | Hua Medicine Limited|Tigermed Consulting Co., Ltd |
Diabetes Mellitus, Type 2
|
September 2015 | Phase 2 |
| NCT03158506 | Hua Medicine Limited |
Healthy Subject
|
March 29, 2017 | Phase 1 |
| NCT04091854 | Majianhua|Nanjing First Hospital, Nanjing Medical University |
Type2 Diabetes Mellitus
|
December 12, 2018 | |
| NCT01952535 | Hua Medicine Limited |
Type II Diabetes Mellitus
|
September 2013 | Phase 1 |
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 : 125 mg/mL ( 270.02 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1602 mL | 10.8008 mL | 21.6015 mL |
| 5 mM | 0.4320 mL | 2.1602 mL | 4.3203 mL |
| 10 mM | 0.2160 mL | 1.0801 mL | 2.1602 mL |
References
- [1] Zhu XX, et al. Dorzagliatin (HMS5552), a novel dual-acting glucokinase activator, improves glycaemic control and pancreatic β-cell function in patients with type 2 diabetes: A 28-day treatment study using biomarker-guided patient selection. Diabetes Obes
- [2] Wang P, et al. Effects of a Novel Glucokinase Activator, HMS5552, on Glucose Metabolism in a Rat Model of Type 2 Diabetes Mellitus. J Diabetes Res. 2017;2017:5812607.