Rosiglitazone maleate CAS NO.155141-29-0
Active Pharmaceutical Ingredients 2025-03-03
Catalog ID80017012
CAS NO.155141-29-0
Purity 98%
MDL NumberMFCD03427306
EINEC Molecular Formula C18H19N3O3S.C4H4O4
Molecular Weight 473.4989
| Aspect | Details |
|---|---|
| Chemical Structure | – Molecular Formula: C₂₂H₂₃N₃O₇S<br>- Molecular Weight: 471.5 |
| Mechanism of Action | – Rosiglitazone activates peroxisome proliferator-activated receptor gamma (PPAR-γ), which regulates fat production and glucose and lipid metabolism.<br>- It improves insulin sensitivity by increasing insulin-stimulated IRS-1/2 expression in skeletal muscle and adipose tissue, followed by increased expression of the GLUT4 glucose transporter. |
| Clinical Uses | – Primarily used to treat type 2 diabetes, either alone or in combination with other oral antidiabetic agents (e.g., metformin or sulfonylureas).<br>- Significantly improves insulin resistance and reduces HbA1c levels by 1% to 2%. |
| Pharmacokinetics | – High bioavailability (99%) and high plasma protein binding (99%).<br>- Metabolized primarily in the liver, with 64% excreted in urine and 22% in feces. |
| Dosage Forms | – Oral tablets, commonly available in 2 mg and 4 mg strengths.<br>- Initial dose is 4 mg daily, which can be increased to 8 mg daily based on glycemic response after 8 to 12 weeks. |
| Adverse Effects | – Common side effects include increased LDL cholesterol, HDL cholesterol, and total cholesterol.<br>- Less common side effects include edema, hypertension, heart failure, myocardial ischemia, diarrhea, and upper respiratory infections.<br>- Women may experience increased risk of fractures and rare cases of macular edema. |
| Storage Conditions | Store in a cool, dry place, protected from moisture and light. |
| Regulatory Status | – Approved by the FDA for medical use in 1999.<br>- Restricted in 2011 due to myocardial infarction risks; restrictions lifted in 2013. |
| Synonyms | – Avandia<br>- BRL 49653<br>- Rosiglitazone maleate |
Disclaimer: The above content is for reference and communication only among industry insiders, and does not guarantee its accuracy or completeness. According to relevant laws and regulations and the regulations of this website, units or individuals who purchase related items should obtain valid qualifications and qualification conditions.
