Dorzagliatin - 98%, high purity , CAS No.1191995-00-2, Allosteric modulator of Glucokinase

Item Number
D413676
Grouped product items
SKUSizeAvailabilityPrice Qty
D413676-5mg
5mg
In stock
$97.90
D413676-25mg
25mg
In stock
$303.90

Carbohydrate Metabolism Activators

Basic Description

SynonymsHY-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
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsDorzagliatin (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 TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeALLOSTERIC MODULATOR
Mechanism of actionAllosteric 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

Product Properties

ALogP2.366
HBD Count3
Rotatable Bond10

Associated Targets(Human)

GCK Tchem Glucokinase (0 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name (2S)-2-[3-(2-chlorophenoxy)-5-oxo-2H-pyrrol-1-yl]-N-[1-[(2R)-2,3-dihydroxypropyl]pyrazol-3-yl]-4-methylpentanamide
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

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

Find and download the COA for your product by matching the lot number on the packaging.

3 results found

Lot NumberCertificate TypeDateItem
K2222465Certificate of AnalysisNov 15, 2022 D413676
K2222516Certificate of AnalysisNov 15, 2022 D413676
K2222552Certificate of AnalysisNov 15, 2022 D413676

Chemical and Physical Properties

SolubilitySolubility (25°C) In vitro DMSO: 92 mg/mL (198.73 mM); Ethanol: 92 mg/mL (198.73 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility92
DMSO(mM) Max Solubility198.734149871471
Water(mg / mL) Max Solubility<1

Safety and Hazards(GHS)

Pictogram(s) GHS07
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.

Related Documents

References

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]

Solution Calculators