Cardinamide is a derivative of sulfonylurea that, when administered orally to normal animals, can result in hypoglycemia [2].

Absorption, Distribution and Excretion
Sulfonylureas are readily absorbed from the gastrointestinal tract. For clinical application, the most important difference between sulfonylureas lies in their duration of action… /Sulfonylureas/ Sulfonylureas primarily bind to plasma proteins and are distributed in the extracellular space. /Sulfonylureas/

---

Metabolism/Metabolites …In the human body, approximately one-third of the excreted dose exists as N-acetylated metabolites. Significant species differences have been found; rabbits produce large amounts of acetyltransferases (AMTs), while monkeys and dogs have very low or no acetylation capacity, and humans are at an intermediate level. These are hydroxylated in the liver into active and inactive products, almost entirely excreted in the urine. /Sulfonylureas/

Interactions
Sodium carbonate can reduce the teratogenic and lethal effects of drugs in rats. Drugs that may increase the risk of hypoglycemia caused by sulfonylureas include other hypoglycemic agents, sulfonamides, propranolol, salicylates, clofibrate, phenylbutazone, probenecid, dicumarol, chloramphenicol, monoamine oxidase inhibitors, and alcohol. /Sulfonylureas/ Alcohol and salicylates may induce hypoglycemic coma in patients taking sulfonylureas due to their direct hypoglycemic effects. Propranolol enhances the hypoglycemic effect of sulfonylureas by interfering with glycogenolysis and glucagon release. /Sulfonylureas/ Simultaneous infusion of a second drug that displaces sulfonylureas in the pancreas can alter sulfonylurea-mediated insulin secretion. Therefore, drug interactions at target organs or receptor sites should be understood to provide adequate drug therapy. For more complete data on interactions of 1-butyl-3-sulfonylureas (a total of 8), please visit the HSDB record page.

[1]. Carbutamide--the first oral antidiabetic. A retrospect. Exp Clin Endocrinol Diabetes. 1998;106(2):149-51.

[2]. Pharmacology of carbutamide (p-aminophenylsulfonyl butylcarbamide). J Pharmacol Exp Ther. 1957 Apr;119(4):468-78.

Carbutamide is a sulfonamide compound, belonging to the benzene family. Carbutamide is a first-generation sulfonylurea drug with hypoglycemic activity. It was one of the earliest sulfonylurea compounds used, but was withdrawn from the market due to its myelotoxicity. The drug has a relatively long half-life. It is a sulfonylurea antidiabetic drug with similar effects and uses to chloropropionamide. (Excerpt from Martindale Pharmacopoeia, 30th edition, page 277) Mechanism of Action: Sulfonylureas stimulate insulin secretion from pancreatic islet tissue. ...Sulfonylureas cause β-cell degranulation, a phenomenon associated with an increased rate of insulin secretion. ...They are effective in insulin-independent diabetic patients whose pancreas still retains the ability to secrete insulin. /Sulfonylureas/ Therapeutic Uses: Hypoglycemic Drugs (Veterinary): Adding carbadamine to the diet of rats for 10-14 days resulted in a significant antithyroid effect. It reduces the uptake of iodine (131) by the thyroid gland and reduces the synthesis of thyroxine. Carbaamide… is an oral sulfonamide hypoglycemic agent used to treat diabetes… Sulfonylureas are only used in patients with insulin-independent diabetes who cannot be treated with diet alone. Sulfonylureas Hypoglycemic Agents

---

Drug Warnings
Hematologic (leukopenia, agranulocytosis, thrombocytopenia, pancytopenia, and hemolytic anemia), skin (rash, photosensitivity), gastrointestinal (nausea, vomiting, rare bleeding), and hepatic (elevated serum alkaline phosphatase, cholestatic jaundice) reactions have been reported. Sulfonylureas To date, increased cardiovascular mortality during sulfonylurea treatment is its main toxic effect. Sulfonylureas Because the liver plays a crucial role in the metabolism of sulfonylureas and the kidneys play a crucial role in the excretion of the drugs and their metabolites, sulfonylureas are contraindicated in patients with hepatic or renal insufficiency. Alcohol intolerance has occasionally occurred in patients taking sulfonylureas. Sulfonylureas are not recommended for pregnant women. Animal studies have shown that high doses of sulfonylureas can cause birth defects. /Sulfonylureas/ For more complete data on drug warnings for 1-butyl-3-sulfonylureas (7 in total), please visit the HSDB records page.

C11H17N3O3S

271.33598

271.099

339-43-5

9564

Crystals

1.266g/cm3

144-145ºC

1.564

3.5

3

4

5

18

356

0

NC1C=CC(S(NC(NCCCC)=O)(=O)=O)=CC=1

VDTNNGKXZGSZIP-UHFFFAOYSA-N

InChI=1S/C11H17N3O3S/c1-2-3-8-13-11(15)14-18(16,17)10-6-4-9(12)5-7-10/h4-7H,2-3,8,12H2,1H3,(H2,13,14,15)

1-(4-aminophenyl)sulfonyl-3-butylurea

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)

DMSO : ~50 mg/mL (~184.27 mM)

Solubility in Formulation 1: ≥ 2.17 mg/mL (8.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 21.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

---

Solubility in Formulation 2: ≥ 2.08 mg/mL (7.67 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.

---

View More

Solubility in Formulation 3: ≥ 2.08 mg/mL (7.67 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.

---

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