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Chemical Structure| 1191995-00-2 Chemical Structure| 1191995-00-2

Structure of Dorzagliatin
CAS No.: 1191995-00-2

Chemical Structure| 1191995-00-2

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Dorzagliatin is a glucokinase activator on glucose metabolism.

Synonyms: HMS5552; RO-5305552; Sinogliatin

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Product Details of Dorzagliatin

CAS No. :1191995-00-2
Formula : C22H27ClN4O5
M.W : 462.93
SMILES Code : CC(C)C[C@H](N1C(C=C(OC2=CC=CC=C2Cl)C1)=O)C(NC3=NN(C[C@@H](O)CO)C=C3)=O
Synonyms :
HMS5552; RO-5305552; Sinogliatin
MDL No. :MFCD22376579
InChI Key :HMUMWSORCUWQJO-QAPCUYQASA-N
Pubchem ID :57920094

Safety of Dorzagliatin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Mouse pancreatic islet β-cells 10 µM 30 minutes To evaluate the effect of Dorzagliatin on glucose-stimulated insulin secretion. Results showed that Dorzagliatin alone had minimal effects on insulin secretion in wild-type and GckKI/+ mouse islets, but significantly enhanced insulin secretion when combined with Exendin-4, particularly in male GckKI/+ mice. bioRxiv [Preprint]. 2024 Nov 11:2024

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c mice PI3Ki-induced hyperglycemic mouse model Oral gavage 10 mg/kg (Dorzagliatin), 0.2 mg/kg (WX390), 25 mg/kg (BYL719) Once daily for 4 weeks To evaluate the effect of Dorzagliatin on PI3Ki-induced hyperglycemia and hyperinsulinemia. Results showed that Dorzagliatin significantly reduced blood glucose levels and C-peptide levels, indicating effective mitigation of hyperinsulinemia. Mol Metab. 2025 Jun;96:102151
Mouse GckKI/+ and GckKI/KI mice Intraperitoneal injection 1 mg/kg Dorzagliatin and 1 nmol/kg Exendin-4 Single dose To evaluate the effects of Dorzagliatin and Exendin-4 on glucose tolerance. Results showed that in male GckKI/+ mice, Dorzagliatin significantly potentiated the action of Exendin-4, restoring glucose tolerance to wild-type levels. In female mice, Exendin-4 alone improved glucose tolerance, but Dorzagliatin did not show additional effects. bioRxiv [Preprint]. 2024 Nov 11:2024

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT04080596 Drug Interaction PHASE1 COMPLETED 2017-12-05 The 2nd Hospital of Jilin Univ... More >>ersity, Changchun, Jilin, 130021, China Less <<
NCT02386982 Type 2 Diabetes PHASE1 COMPLETED 2025-05-15 The 1st Betuhune Hospital of J... More >>ilin University, Changchun, China Less <<
NCT06671340 Diabetes Mellitus|Prediabetes ... More >>/ Type 2 Diabetes Less << NOT_YET_RECRUITING 2026-01-31 Phase 1 Clinical Trial Centre,... More >> Hong Kong, Hong Kong Less <<
NCT04091854 Type2 Diabetes Mellitus UNKNOWN 2025-03-22 Nanjing First hospital, Nanjin... More >>g, Jiangsu, China Less <<
NCT04080609 Drug Interaction PHASE1 COMPLETED 2018-04-17 Central Hospital of Xuhui Dist... More >>rict, Shanghai, Shanghai, 201203, China Less <<
NCT04426708 Type 2 Diabetes Mellitus PHASE1 COMPLETED 2020-07-03 West China Hospital of Sichuan... More >> University, Chengdu, Sichuan, 610000, China Less <<
NCT03158506 Healthy Subject PHASE1 COMPLETED 2017-04-06 Celerion, Lincoln, Nebraska, 6... More >>8502, United States Less <<
NCT04324424 Type 2 Diabetes Mellitus PHASE1 COMPLETED 2019-09-30 West China Hospital of Sichuan... More >> University, Chengdu, Sichuan, 610000, China Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.16mL

0.43mL

0.22mL

10.80mL

2.16mL

1.08mL

21.60mL

4.32mL

2.16mL

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