Glipizide

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Cat Number

API29094619

CAS Number

29094-61-9

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Product Detail Description Scientific Support Customer Q&A

CAS Number

29094-61-9

EINECS

249-427-6

Storage

Store at 2-8℃

Synonyms

Glucotrol; Glydiazinamide; Glibenese; Melizide; Minidiab

Molecular Formula

C21H27N5O4S

Molecular Weight

445.5

Smiles

CC1=CN=C(C=N1)C(=O)NCCC2=CC=C(C=C2)S(=O)(=O)NC(=O)NC3CCCCC3

Appearance

White to off-white crystalline powder

Melting Point

208-209℃

Boiling Point

676℃

Relative Density

1.34

General Description

Glipizide is an oral sulfonylurea hypoglycemic agent of the second generation, used as adjunctive therapy in the management of type 2 diabetes mellitus. It is available in immediate-release and extended-release tablets, with the latter providing once-daily dosing. This agent is characterized by its rapid absorption and relatively short duration of action compared to other sulfonylureas such as glyburide.

Mechanism of Action

Glipizide lowers blood glucose primarily by stimulating insulin release from the beta cells of the pancreatic islets. It binds to the sulfonylurea receptor (SUR1) on the ATP-sensitive potassium channel, closing the channel and causing membrane depolarization. This triggers calcium influx via voltage-gated calcium channels, leading to exocytosis of stored insulin granules. The effect is dependent on functioning beta cells and requires the presence of glucose.

Application

It is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus. The extended-release formulation allows for once-daily administration, typically with breakfast. Glipizide is generally preferred in elderly patients or those with renal impairment because it is metabolized to inactive products and has a lower risk of prolonged hypoglycemia compared to glyburide. Weight gain and hypoglycemia remain the most common adverse effects.

This mechanistic study shows that glipizide, an oral hypoglycemic agent, overcomes TRAIL resistance in human lung adenocarcinoma cells. Pretreatment with glipizide downregulated p‑Akt and p‑mTOR, activated autophagic flux (increased LC3‑II conversion, decreased p62), and enhanced TRAIL‑mediated apoptosis. Blocking autophagy with a specific inhibitor or ATG5 siRNA abolished glipizide’s sensitizing effect. The authors demonstrate that glipizide inhibits the Akt/mTOR pathway, thereby promoting autophagy flux and sensitizing cancer cells to TRAIL. They propose glipizide as a potential combination partner with TRAIL protein for treating TRAIL‑resistant tumors.

Fig. 1 Glipizide sensitizes TRAIL-mediated apoptosis in lung adenocarcinomacells. (Nazim UM, et al., 2017)

References

Nazim UM, et al. Glipizide sensitizes lung cancer cells to TRAIL-induced apoptosis via Akt/mTOR/autophagy pathways. Oncotarget. 2017; 8(59):100021-100033.

Does Glipizide discolor upon exposure to light or air?

Yes, it is sensitive to light and may yellow over time. Storage in light-resistant, airtight containers is recommended to prevent oxidative discoloration.

What is the recommended storage humidity for Glipizide?

Store below 60% RH. It is not highly hygroscopic, but prolonged exposure to high humidity can lead to hydrolysis of the sulfonylurea moiety.

Is Glipizide stable in solid oral dosage forms with common excipients?

Yes, it shows good compatibility with lactose, microcrystalline cellulose, and starch. We provide stability data for direct compression and wet granulation formulations.

How is the degradation product sulfonamide impurity quantified?

Using a stability-indicating HPLC method, we monitor the formation of sulfonamide-related compounds, ensuring they stay within ICH qualification limits.