| 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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Purity: ≥98%
Dorzagliatin (RO-5305552; HMS-5552; sinogliatin) is an investigational antidiabetic agent acting as a dual-acting glucokinase activator (GKA) that is able to improves glycaemic control and pancreatic β-cell function in type 2 diabete. As of 2022 Oct 8, Dorzagliatin gained approval from the Chinese FDA (NMPA) for treating types II diabetes. Glucokinase (GK) plays a critical role in the control of whole-body glucose homeostasis. The novel GKA, HMS5552, exerts antidiabetic effects on the liver and pancreas by improving GK activity and insulin resistance, which holds promise as a novel drug for the treatment of T2DM patients.
| 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].
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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. |
| References |
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| Additional Infomation |
Dorzagliatin is under investigation in clinical trial NCT03173391 (Long-term Efficacy and Safety of HMS5552 in T2DM).
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| 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
|
| 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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