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| 500mg |
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Purity: ≥98%
Gliclazide (S-1702; trade names Diamicron among others), a sulfonylurea insulin secretagogue, is an approved medication for the treatment of type 2 diabetes. It acts as a potent and ATP-sensitive potassium currents blocker with an IC50 of 184 nM, and can stimulate β cells of the pancreas to release insulin.
| ln Vitro |
Gliclazide (S1702) further explains the mechanism underlying its hypoglycemic effect: the drug's insulinotropic sulfonylurea effect is further enhanced by the observed improvements in GLUT4 translocation and insulin sensitivity, which counteract the insulin resistance that hydrogen peroxide causes in 3T3L1 adipocytes [1]. Gliclazide demonstrated a significant reduction in efficacy in cardiac and smooth muscle, with IC50s of 19.5 +/- 5.4 micromol/l (n = 6–12) and 37.9 +/– 1.0 micromol/l (n = 5–10), respectively. However, it was significantly more effective in blocking whole-cell beta-cell KATP currents in this latter tissue. The drug affected whole-cell KATP currents in all three tissues, but its effects were quickly reversible. Gliclazide (1 micromol/l) on beta-cells led to a maximum of 66 +/- 13% inhibition (n=5) in inside-out patches, while over 98% block was produced in the whole-cell configuration. is a high-potency sulphonylurea that exhibits over heart and smooth muscle specificity for the pancreatic beta-cell KATP channel. It stands apart from glibenclamide in this regard[2].
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| References |
[1]. Shimoyama, T., et al., Gliclazide protects 3T3L1 adipocytes against insulin resistance induced by hydrogen peroxide with restoration of GLUT4 translocation. Metabolism, 2006. 55(6): p. 722-30.
[2]. Lawrence, C.L., et al., Gliclazide produces high-affinity block of KATP channels in mouse isolated pancreatic beta cells but not rat heart or arterial smooth muscle cells. Diabetologia, 2001. 44(8): p. 1019-25. |
| Molecular Formula |
C15H21N3O3S
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| Molecular Weight |
323.41
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| CAS # |
21187-98-4
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| Related CAS # |
Gliclazide-d4;1185039-30-8
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| SMILES |
S(C1C([H])=C([H])C(C([H])([H])[H])=C([H])C=1[H])(N([H])C(N([H])N1C([H])([H])C2([H])C([H])([H])C([H])([H])C([H])([H])C2([H])C1([H])[H])=O)(=O)=O
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| InChi Key |
BOVGTQGAOIONJV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H21N3O3S/c1-11-5-7-14(8-6-11)22(20,21)17-15(19)16-18-9-12-3-2-4-13(12)10-18/h5-8,12-13H,2-4,9-10H2,1H3,(H2,16,17,19)
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| Chemical Name |
1-(3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrol-2-yl)-3-(4-methylphenyl)sulfonylurea
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.73 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 25.0 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: ≥ 2.5 mg/mL (7.73 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 25.0 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: ≥ 2.5 mg/mL (7.73 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 | 3.0921 mL | 15.4603 mL | 30.9205 mL | |
| 5 mM | 0.6184 mL | 3.0921 mL | 6.1841 mL | |
| 10 mM | 0.3092 mL | 1.5460 mL | 3.0921 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00738088 | Terminated | Drug: gliclazide | Diabetes Mellitus, Type 2 | NHS Tayside | June 2007 | Phase 4 |
| NCT04132934 | Completed | Type 2 Diabetes | Servier Affaires Médicales | March 11, 2019 | ||
| NCT06085703 | Recruiting | Drug: Henagliflozin Drug: Gliclazide |
Type 2 Diabetes Mellitus Mild Cognitive Impairment |
The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School |
September 1, 2023 | Not Applicable |
| NCT06222476 | Not yet recruiting | Drug: Dorzagliatin Drug: Gliclazide |
Diabetic Nephropathy Type 2 | Yan Bi | February 20, 2024 | Not Applicable |
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