API Rosiglitazone

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Product Overview

Rosiglitazone (also known by brand names Avandia, Anxiantian) is a pharmaceutical compound developed by GlaxoSmithKline (GSK). It is a selective PPARγ agonist belonging to the thiazolidinedione (TZD) class of insulin sensitizer drugs. This compound is used for the treatment of type 2 diabetes mellitus and has been subject to regulatory restrictions due to cardiovascular risk concerns.

Chemical Specifications

Rosiglitazone has the following well-defined chemical specifications:

CAS Number: 122320-73-4

Molecular Formula: C₁₈H₁₉N₃O₃S

Molecular Weight: 357.43 g/mol

Chemical Name: 5-

EINECS Number: Not specified in search results

MDL Number: MFCD00871760

RTECS Number: XJ5813850

Key Properties

Physical Appearance: White to off-white crystalline solid or powder

Melting Point: 153-155°C

Boiling Point: 585°C

Solubility:

Soluble in DMSO (25 mg/mL at 25°C or 45 mg/mL)

Soluble in DMF and methanol

Insoluble in water

Purity: ≥98% to ≥99% depending on manufacturer specifications

Mechanism Classification: Selective PPARγ agonist with EC50 of 43-60 nM and Kd of approximately 40 nM

Alternative Names: BRL 49653

Mechanism of Action

Rosiglitazone functions as a peroxisome proliferator-activated receptor gamma (PPARγ) agonist. The compound binds to PPARγ and activates gene transcription related to adipocyte differentiation, thereby enhancing insulin sensitivity. The drug works by:

Increasing adipocyte differentiation

Regulating adipogenesis and glucose metabolism

Improving insulin resistance without directly affecting insulin production

Lowering blood glucose levels through enhanced insulin sensitivity

Compared to pioglitazone, rosiglitazone demonstrates approximately 30-fold higher binding affinity for PPARγ.

Clinical Applications

FDA-Approved Indications

Type 2 Diabetes Mellitus: Used as monotherapy or in combination with metformin or sulfonylurea agents

Cardiovascular Protection: Under certain restricted circumstances for patients with diabetes and cardiovascular disease

Research Applications

Rosiglitazone is widely used in scientific research for studies related to:

Diabetes and metabolic disease models

Obesity research

Aging studies

Ovarian cancer research

Neuroprotection and anti-inflammatory studies

Recommended Dosage

For human therapeutic use:

Initial Dose: 4 mg once daily

Maximum Dose: 8 mg per day

Administration: Can be given once daily or divided into twice daily dosing

For research use:

Powder Form: Available in 50mg, 100mg, 250mg, 500mg, and 1g specifications

Solution Form: 1 mL (10 mM in DMSO)

Other Forms: 25mg, 100mg, 200mg packages available

Safety Profile

Common Side Effects

Weight gain

Edema/water retention

Hypoglycemia, especially when combined with sulfonylureas or insulin

Anemia

Increased risk of bone fractures, particularly in females

Serious Risks

Heart Failure: Rosiglitazone carries risk of exacerbating or causing heart failure

Cardiovascular Death Risk: FDA has restricted use due to increased cardiovascular mortality risk

Liver Toxicity: Hepatotoxicity concerns require liver function monitoring

Macular Edema: Risk of macular edema

Bone Loss: Increases risk of bone mineral density loss in postmenopausal women

Contraindications

Type 1 diabetes mellitus

Severe heart failure

Liver disease or hepatic impairment

Pregnancy

Drug Interactions

Rosiglitazone has been studied in combination with:

Metformin

Sulfonylureas

Pioglitazone

Other antidiabetic medications

Combination with sulfonylureas or insulin may increase the risk of hypoglycemia.

Storage and Handling

Recommended Storage Conditions:

Powder form: Store at 2-8°C for up to 2 years

Alternative: Store at -20°C for powder for 3 years

In DMSO or other solvent: Store at 2-4°C for two weeks, or at -20°C for six months

Protect from light and moisture

Transportation:

Room temperature shipping available

Blue ice for certain formulations

Cold transport for some suppliers

Regulatory Status

Rosiglitazone has been subject to significant regulatory restrictions in various jurisdictions due to cardiovascular risk concerns:

FDA Restrictions: Use restricted in some countries; only recommended as alternative when other glucose-lowering medications fail

Marketing Status: Remains available but with enhanced warning requirements

Brand Names: Avandia (Rosiglitazone maleate)

Important Notes

This prescription medication requires healthcare professional supervision

Regular monitoring of liver function and cardiac status is essential

Patients with renal impairment may require dose adjustments

Elderly patients and those with liver or kidney dysfunction should be monitored closely

The drug should not be used in patients with severe heart failure

For research reference standards, the product is intended for laboratory research and analytical use only