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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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D413676-5mg | 5mg | In stock | $97.90 | |
D413676-25mg | 25mg | In stock | $303.90 |
Carbohydrate Metabolism Activators
Synonyms | HY-109030 | AKOS030527745 | Sinogliatin | (2S)-2-[3-(2-chlorophenoxy)-5-oxo-2H-pyrrol-1-yl]-N-[1-[(2R)-2,3-dihydroxypropyl]pyrazol-3-yl]-4-methylpentanamide | MFCD22376579 | 1191995-00-2 | BD167920 | DB15123 | HMS5552 | HMS-5552 | KBioSS_000661 | (S)-2-(4 |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Dorzagliatin (HMS-5552, RO-5305552, Sinogliatin) is a dual-acting glucokinase (GK) activator that improves glycaemic control and pancreatic β-cell function in patients with type 2 diabetes. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | ALLOSTERIC MODULATOR |
Mechanism of action | Allosteric modulator of Glucokinase |
Product Description | Information Dorzagliatin Dorzagliatin (HMS-5552, RO-5305552, Sinogliatin) is a dual-acting glucokinase (GK) activator that improves glycaemic control and pancreatic β-cell function in patients with type 2 diabetes. Targets glucokinase |
ALogP | 2.366 |
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HBD Count | 3 |
Rotatable Bond | 10 |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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IUPAC Name | (2S)-2-[3-(2-chlorophenoxy)-5-oxo-2H-pyrrol-1-yl]-N-[1-[(2R)-2,3-dihydroxypropyl]pyrazol-3-yl]-4-methylpentanamide |
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INCHI | 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 |
InChi Key | HMUMWSORCUWQJO-QAPCUYQASA-N |
Canonical SMILES | CC(C)CC(C(=O)NC1=NN(C=C1)CC(CO)O)N2CC(=CC2=O)OC3=CC=CC=C3Cl |
Isomeric SMILES | CC(C)C[C@@H](C(=O)NC1=NN(C=C1)C[C@H](CO)O)N2CC(=CC2=O)OC3=CC=CC=C3Cl |
Alternate CAS | 1191995-00-2 |
PubChem CID | 57920094 |
MeSH Entry Terms | (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;Dorzagliatin;HMS5552;sinogliatin |
Molecular Weight | 462.93 |
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Solubility | Solubility (25°C) In vitro DMSO: 92 mg/mL (198.73 mM); Ethanol: 92 mg/mL (198.73 mM); Water: Insoluble; |
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DMSO(mg / mL) Max Solubility | 92 |
DMSO(mM) Max Solubility | 198.734149871471 |
Water(mg / mL) Max Solubility | <1 |
Pictogram(s) | GHS07 |
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Signal | Warning |
Hazard Statements | H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation |
Precautionary Statements | P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. |
1. Grimsby J, Sarabu R, Corbett WL, Haynes NE, Bizzarro FT, Coffey JW, Guertin KR, Hilliard DW, Kester RF, Mahaney PE et al.. (2003) Allosteric activators of glucokinase: potential role in diabetes therapy.. Science, 301 (5631): (370-3). [PMID:12869762] [10.1021/op500134e] |
2. Wang P, Liu H, Chen L, Duan Y, Chen Q, Xi S. (2017) Effects of a Novel Glucokinase Activator, HMS5552, on Glucose Metabolism in a Rat Model of Type 2 Diabetes Mellitus.. J Diabetes Res, 2017 (13): (5812607). [PMID:28191470] [10.1021/op500134e] |
3. Bloomgarden Z. (2019) Glucokinase and the potential of glucokinase activation in type 2 diabetes.. J Diabetes, 11 (8): (626-627). [PMID:31013387] [10.1021/op500134e] |
4. Zhu XX, Zhu DL, Li XY, Li YL, Jin XW, Hu TX, Zhao Y, Li YG, Zhao GY, Ren S et al.. (2018) 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 Metab, 20 (9): (2113-2120). [PMID:29707866] [10.1021/op500134e] |
5. Toulis KA, Nirantharakumar K, Pourzitaki C, Barnett AH, Tahrani AA. (2020) Glucokinase Activators for Type 2 Diabetes: Challenges and Future Developments.. Drugs, 80 (5): (467-475). [PMID:32162273] [10.1021/op500134e] |
6. Sharma P, Singh S, Sharma N, Singla D, Guarve K, Grewal AS. (2022) Targeting human Glucokinase for the treatment of type 2 diabetes: an overview of allosteric Glucokinase activators.. J Diabetes Metab Disord, 21 (1): (1129-1137). [PMID:35673438] [10.1021/op500134e] |