- Dorzagliatin
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- $34.00 / 1mg
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2026-01-20
- CAS:1191995-00-2
- Min. Order:
- Purity: 99.45%
- Supply Ability: 10g
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| | Dorzagliatin Basic information |
| Product Name: | Dorzagliatin | | Synonyms: | (S)-2-(4-(2-chlorophenoxy)-2-oxo-2,5-dihydro-1H-pyrrol-1-yl)-N-(1-((R)-2,3-dihyd;(S)-2-[4-(2-chloro-phenoxy)-2-oxo-2,5-dihydro-pyrrol-1-yl]-4-methyl-pentanoic acid [1-((R)-2,3-dihydroxy-propyl)-1H-pyrazol-3-yl]-amide;(S)-2-(4-(2-chlorophenoxy)-2-oxo-2,5-dihydro-1H-pyrrol-1-yl)-N-(1-((R)-2,3-dihydroxypropyl)-1H-pyrazol-3-yl)-4-MethylpentanaMide;RO-5305552;DORZAGLIATIN;1191995-00-2;DORZAGLIATIN; SINOGLIATIN ;HMS5552; RO5305552;1H-Pyrrole-1-acetamide, 4-(2-chlorophenoxy)-N-[1-[(2R)-2,3-dihydroxypropyl]-1H-pyrazol-3-yl]-2,5-dihydro-α-(2-methylpropyl)-2-oxo-, (αS)-;diabetes,inhibit,β-cell,Hexokinase IV,Inhibitor,glycaemic,type 2,Hexokinase D,Glucokinase,Dorzagliatin,pancreatic,HMS-5552,HMS 5552;Dorzagliatin (Synonyms: HMS5552) | | CAS: | 1191995-00-2 | | MF: | C22H27ClN4O5 | | MW: | 462.93 | | EINECS: | | | Product Categories: | | | Mol File: | 1191995-00-2.mol |  |
| | Dorzagliatin Chemical Properties |
| Boiling point | 761.7±60.0 °C(Predicted) | | density | 1.38±0.1 g/cm3(Predicted) | | solubility | DMSO:108.5(Max Conc. mg/mL);234.38(Max Conc. mM)
Ethanol:92.0(Max Conc. mg/mL);198.73(Max Conc. mM) | | form | Solid | | pka | 12.84±0.70(Predicted) | | color | White to off-white |
| | Dorzagliatin Usage And Synthesis |
| Description | Dorzagliatin (trade name HuaTangNing) is a first-in-class small molecule oral glucokinase activator (GKA) developed by Hua Medicine for the treatment of diabetic nephropathy (DKD), type 1 diabetes mellitus (T1DM) and type 2 diabetes mellitus (T2DM). Dorzagliatin was first approved in China in September 2022 as a monotherapy or in combination with metformin, an antidiabetic drug, for adults with type 2 diabetes. | | Uses | Dorzagliatin (HMS5552), a dual-acting glucokinase (GK) activator, improves glycaemic control and pancreatic β-cell function in type 2 diabetes[1]. | | Mechanism of action | The mechanism of action of dolagliflozin is through the activation of glucokinase, an enzyme that plays a key role in blood sugar regulation. By increasing the activity of glucokinase, dolagliflozin helps improve blood sugar control, especially in situations where blood sugar rises after a meal. | | Synthesis | First, ethyl 2-butynoate was subjected to base-mediated olefination of 2-chlorophenol (18.5) to afford the ester 18.6 (Figure 5.2.2). Subsequent bromination with NBS and AIBN afforded the allylic bromide 18.7. Next, L-leucine methyl ester hydrochloride (18.8) was added to the base to afford the free amine, which underwent allylation with the bromide 18.7. The acid 18.9 was generated via cyclization-condensation and hydrolysis with NaOH. EDCI and HOBt promoted the formation of the final amide bond to afford the amide 18.10, and the 1,2-diol was subjected to acid-mediated acetone deprotection to afford dogliflozin (18) on a 100 kg scale.
 | | 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. | 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. |
| | 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 DOI:10.1111/dom.13338
[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. DOI:10.1155/2017/5812607 |
| | Dorzagliatin Preparation Products And Raw materials |
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