| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Dorzagliatin is a dual-acting glucokinase (GK) activator. It activates glucokinase, a key enzyme in glucose metabolism, by binding to an allosteric site. This increases glucose uptake and utilization in the liver and pancreas, enhancing insulin secretion and improving glycemic control.
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| ln Vitro |
In vitro, Dorzagliatin is a glucokinase activator that improves GK activity. It increases the affinity of glucokinase for glucose, enhancing glucose phosphorylation and metabolism. The compound's dual-acting mechanism involves activation of glucokinase in both the liver and pancreas, promoting glucose utilization and insulin secretion.
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| ln Vivo |
Dorzagliatin has a hypoglycemic impact on blood glucose levels of diabetes cholesterol (low dose: 10 mg/kg, high dose: 30 mg/kg; intragastric formulation; daily at 8:00 a.m. for one month) [2].
Dorzagliatin has been shown to decrease blood glucose levels and improve GK activity and insulin resistance in vivo. It improves glycaemic control and pancreatic β-cell function in type 2 diabetes. The compound is a novel oral antidiabetic drug developed for the treatment of type 2 diabetes mellitus. |
| Enzyme Assay |
In vitro enzyme assays for Dorzagliatin typically measure its ability to activate glucokinase activity. Recombinant glucokinase is incubated with glucose and ATP in the presence of increasing concentrations of the compound. The formation of glucose-6-phosphate is measured using a coupled enzyme assay (e.g., glucose-6-phosphate dehydrogenase). EC50 values are calculated from dose-response curves. The compound's selectivity for glucokinase over other hexokinases is assessed.
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| Cell Assay |
Cell-based assays for Dorzagliatin involve treating pancreatic β-cells or hepatocytes with the compound and measuring glucose metabolism and insulin secretion. β-cells are incubated with glucose and the compound, and insulin secretion is measured by ELISA. Hepatocytes are treated with the compound, and glucose uptake and glycogen synthesis are assessed. The compound's effects on glucose-stimulated insulin secretion and hepatic glucose metabolism are quantified.
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| Animal Protocol |
Animal/Disease Models: Male Sprague -Dawley (SD) rat (age approximately 6-8 weeks, body weight 200-230 g) [2 doses: low dose (10 mg/kg) and high dose (30 mg/kg)
Route of Administration: intragastric (po) (po)administration (ig)); daily (8:00 a.m.) for one month Experimental Results: Produces a hypoglycemic effect on blood sugar levels. In vivo animal studies for Dorzagliatin typically involve administering the compound to rodent models of type 2 diabetes (e.g., db/db mice, Zucker diabetic fatty rats). Blood glucose levels are measured over time. Oral glucose tolerance tests (OGTT) are performed. Insulin and C-peptide levels are measured. Pancreatic β-cell function is assessed by glucose-stimulated insulin secretion. The compound's efficacy in improving glycemic control is evaluated. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Dorzagliatin are characteristic of orally bioavailable small molecules. The compound is absorbed following oral administration and distributed to tissues. It has a half-life suitable for twice-daily dosing. Metabolism occurs primarily in the liver via CYP450 enzymes. Excretion occurs through biliary and renal pathways. The compound's pharmacokinetics have been characterized in preclinical and clinical studies.
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| Toxicity/Toxicokinetics |
Toxicological profile of Dorzagliatin has been evaluated in preclinical and clinical studies. The compound is generally well-tolerated. Common side effects include mild gastrointestinal disturbances and hypoglycemia at high doses. The compound's safety profile supports its use as an antidiabetic agent. Long-term safety data are being accumulated from ongoing clinical trials.
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| References |
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| Additional Infomation |
Dorzagliatin is being investigated in the clinical trial NCT03173391 (Long-term efficacy and safety of HMS5552 in the treatment of type 2 diabetes).
Dorzagliatin is a first-in-class glucokinase activator that has completed Phase III clinical trials for the treatment of type 2 diabetes in China. It is a dual-acting GKA that improves both glycemic control and β-cell function. The compound represents a novel approach to diabetes treatment by targeting the glucose sensor glucokinase. |
| Molecular Formula |
C22H27CLN4O5
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|---|---|
| Molecular Weight |
462.931
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| Exact Mass |
462.166
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| CAS # |
1191995-00-2
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| Related CAS # |
1191995-14-8 (HCl);1191995-00-2;
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| PubChem CID |
57920094
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
761.7±60.0 °C at 760 mmHg
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| Flash Point |
414.5±32.9 °C
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| Vapour Pressure |
0.0±2.7 mmHg at 25°C
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| Index of Refraction |
1.631
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| LogP |
2.78
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
32
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| Complexity |
691
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC(C)C[C@@H](C(=O)NC1=NN(C=C1)C[C@H](CO)O)N2CC(=CC2=O)OC3=CC=CC=C3Cl
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| InChi Key |
HMUMWSORCUWQJO-QAPCUYQASA-N
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| InChi Code |
InChI=1S/C22H27ClN4O5/c1-14(2)9-18(22(31)24-20-7-8-26(25-20)11-15(29)13-28)27-12-16(10-21(27)30)32-19-6-4-3-5-17(19)23/h3-8,10,14-15,18,28-29H,9,11-13H2,1-2H3,(H,24,25,31)/t15-,18+/m1/s1
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| Chemical Name |
(2S)-2-[4-(2-chlorophenoxy)-2-oxo-2,5-dihydro-1H-pyrrol-1-yl]-N-{1-[(2R)-2,3-dihydroxypropyl]-1H-pyrazol-3-yl}-4-methylpentanamide
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| Synonyms |
Dorzagliatinsinogliatin, HMS 5552RO-5305552 HMS-5552 RO5305552 HMS5552RO 5305552
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~270.02 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.49 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 (4.49 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 (4.49 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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.
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