Absorption, Distribution and Excretion
Rapid and complete absorption after oral administration. Biological Half-Life 4 hours.

Protein binding
90% binds to plasma proteins.

[1]. Glymidine. Br Med J. 1967;2(5555):817.

Glymidine is a sulfonamide compound, chemically named N-(pyrimidin-2-yl)benzenesulfonamide, where the 5-position of the pyrimidine ring is replaced by a 2-methoxyethoxy group. It is a hypoglycemic drug used to treat diabetes. Glymidine has a hypoglycemic effect and belongs to the pyrimidine, sulfonamide, and diether classes of compounds. It is the conjugate acid of Glymidine (1-). Glymidine, used in combination with dietary therapy, lowers blood glucose by increasing pancreatic insulin secretion and enhancing peripheral tissue sensitivity to insulin. The mechanism of action of Glymidine in lowering blood glucose appears to depend on stimulating the release of insulin from functional pancreatic β-cells and increasing peripheral tissue sensitivity to insulin. Glymidine may bind to ATP-sensitive potassium channel receptors on the surface of pancreatic cells, reducing potassium ion conductance and leading to cell membrane depolarization. Membrane depolarization stimulates calcium ion influx through voltage-gated calcium channels. The increased intracellular calcium ion concentration induces insulin secretion. It is often used in combination with insulin to treat non-insulin-dependent (type 2) diabetes. Glymidine is a sulfadiazine derivative, also known as glycine diazine, with hypoglycemic activity. Similar to sulfonylureas, Glymidine lowers blood glucose levels by increasing insulin release from pancreatic β-cells and enhancing peripheral tissue sensitivity to insulin. Drug Indications Glymidine is used in combination with insulin to treat non-insulin-dependent (type 2) diabetes. Mechanism of Action The mechanism of action of Glymidine in lowering blood glucose appears to be through stimulating insulin release from functional pancreatic β-cells and enhancing peripheral tissue sensitivity to insulin. Glymidine may bind to ATP-sensitive potassium channel receptors on the surface of pancreatic islet cells, reducing potassium conductance and leading to cell membrane depolarization. Cell membrane depolarization stimulates calcium ion influx through voltage-sensitive calcium channels. Increased intracellular calcium ion concentration leads to increased fusion of insulin granules with the cell membrane, thereby increasing proinsulin secretion.

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Pharmacodynamics
Glycine, when used in combination with dietary therapy, lowers blood sugar by increasing pancreatic insulin secretion and improving peripheral tissue sensitivity to insulin.

C13H15N3O4S

309.34

309.078

339-44-6

9565

Typically exists as solid at room temperature

1.354g/cm3

515.1ºC at 760mmHg

220-223

265.4ºC

1.588

2.456

1

7

7

21

385

0

COCCOC1=CN=C(NS(C2C=CC=CC=2)(=O)=O)N=C1

QFWPJPIVLCBXFJ-UHFFFAOYSA-N

InChI=1S/C13H15N3O4S/c1-19-7-8-20-11-9-14-13(15-10-11)16-21(17,18)12-5-3-2-4-6-12/h2-6,9-10H,7-8H2,1H3,(H,14,15,16)

N-[5-(2-methoxyethoxy)pyrimidin-2-yl]benzenesulfonamide

Glycodiazine; GLYMIDINE; Glycodiazine

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.)