Glimepirid active metabolite

Metabolites/Metabolites
Cyclohexylhydromethylglimepiride is a known human metabolite of glimepiride.

[1]. Langtry, et al. Glimepiride. A review of its use in the management of type 2 diabetes mellitus. Drugs 55(4), 563-584 (1998).

Glimepiride is a sulfonylurea drug that stimulates the release of insulin from pancreatic β-cells and may act through extrapancreatic mechanisms. It is used once daily to treat type 2 (non-insulin-dependent) diabetes patients whose blood glucose cannot be controlled by diet and exercise alone, and can also be used in combination with insulin for patients who have failed sulfonylurea therapy. The peak hypoglycemic effect of glimepiride occurs within 4 hours after administration. Compared to glibenclamide, glimepiride has fewer and milder effects on cardiovascular variables. Pharmacokinetics are largely unaffected in elderly patients or those with kidney or liver disease. Few drug interactions have been reported with glimepiride. For patients with type 2 diabetes, the effective dose range of glimepiride is 0.5 to 8 mg/day, but there is little difference in efficacy between doses of 4 mg/day and 8 mg/day. In a 1-year study, the efficacy of glimepiride was similar to that of glibenclamide and glipizide. However, in the first few weeks of treatment, glimepiride appeared to lower blood glucose more rapidly than glipizide. A 14-week study compared the efficacy of glimepiride and gliclazide in patients with good baseline glycemic control, showing no difference in efficacy. For patients who achieved target fasting blood glucose (≤7.8 mmol/L) due to failure of sulfonylurea therapy, glimepiride combined with insulin was comparable in efficacy to insulin combined with placebo, although the glimepiride group required a lower insulin dose and had a faster onset of action. While glimepiride monotherapy was generally well-tolerated, hypoglycemia occurred in 10% to 20% of patients treated for ≤1 year, and in ≥50% of patients treated with insulin combination therapy for 6 months. Pooled clinical trial data suggest that the incidence of hypoglycemia with glimepiride may be lower than with glibenclamide, especially in the first month of treatment. The usual starting dose is 1 mg/day, followed by dose adjustments every 1 to 2 weeks based on glycemic control, with a common dose range of 1 to 4 mg/day (maximum dose in the UK is 6 mg/day, and in the US it is 8 mg/day). Conclusion: Glimepiride is a convenient alternative to sulfonylureas for patients with type 2 diabetes whose diet control is poor. Its potential tolerability advantage and its use in combination with other oral hypoglycemic agents need further investigation. It has been reported that when glimepiride is used in combination with insulin, it can also reduce the exogenous insulin requirement in patients who have failed secondary sulfonylurea therapy. [1]

C24H34N4O6S

506.61

600177-94-4

Typically exists as solids at room temperature

1.3±0.1 g/cm3

1.613

0.93

OCC1CCC(NC(NS(C2C=CC(CCNC(N3CC(C)=C(CC)C3=O)=O)=CC=2)(=O)=O)=O)CC1

Hydroxyglimepiride; Hydroxy-glimepiride; 127554-89-6; DTXSID20155602; 3-Ethyl-2,5-dihydro-N-(2-(4-(((((4-(hydroxymethyl)cyclohexyl)amino)carbonyl)amino)sulfonyl)phenyl)ethyl)-4-methyl-2-oxo-1H-pyrrole-1-carboxamide; 1H-Pyrrole-1-carboxamide, 3-ethyl-2,5-dihydro-N-(2-(4-(((((4-(hydroxymethyl)cyclohexyl)amino)carbonyl)amino)sulfonyl)phenyl)ethyl)-4-methyl-2-oxo-; DTXCID4078093; ...; 600177-94-4;

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)