Rosiglitazone maleate CAS NO.155141-29-0
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Category：Active Pharmaceutical Ingredients MOQ:100KG Shipped directly from China
Introduction
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 |
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