Dapagliflozin 99% Purity SGLT2 Inhibitor CAS 461432-26-8 Antidiabetic API Pharmaceutical Grade

Product Overview

Dapagliflozin is an orally active sodium-glucose cotransporter 2 (SGLT2) inhibitor used for the treatment of type 2 diabetes mellitus, heart failure, and chronic kidney disease. Marketed under the brand name Farxiga (Forxiga in Europe), dapagliflozin was the first SGLT2 inhibitor approved by the FDA in January 2014. By inhibiting SGLT2 in the renal proximal tubules, dapagliflozin reduces glucose reabsorption and increases urinary glucose excretion, lowering blood glucose levels independent of insulin action. Beyond glycemic control, dapagliflozin has demonstrated significant cardiovascular and renal protective benefits, expanding its therapeutic scope.

Chemically, dapagliflozin is (2S,3R,4R,5S,6R)-2-[4-chloro-3-(4-ethoxybenzyl)phenyl]-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol with the molecular formula C₂₁H₂₅ClO₆ and a molecular weight of 408.87 g/mol. It is a white to off-white crystalline powder with solubility in organic solvents. The compound exhibits high selectivity for SGLT2 over SGLT1 and favorable pharmacokinetic properties including good oral bioavailability.

Mechanism of Action

Dapagliflozin exerts its therapeutic effects through SGLT2 inhibition:

• SGLT2 Inhibition: Selectively inhibits sodium-glucose cotransporter 2 (SGLT2) in the proximal renal tubules, reducing renal glucose reabsorption

• Increased Urinary Glucose Excretion: Lowers the renal threshold for glucose, leading to increased glucose excretion in urine

• Insulin-independent Glucose Lowering: Reduces blood glucose levels independent of insulin secretion and sensitivity

• Cardiovascular Protection: Reduces preload and afterload, lowers blood pressure, and provides direct cardiac benefits

• Renal Protection: Reduces intraglomerular pressure and proteinuria, slowing progression of chronic kidney disease

Research Applications & Market Significance

Dapagliflozin has transformed the treatment landscape for diabetes and cardio-renal diseases:

• Type 2 Diabetes Mellitus: First-line or second-line treatment for type 2 diabetes as monotherapy or in combination with other antidiabetic agents

• Heart Failure: Approved for heart failure with reduced ejection fraction (HFrEF) and heart failure with preserved ejection fraction (HFpEF)

• Chronic Kidney Disease: Indicated for slowing progression of CKD in patients with and without diabetes

• Cardiovascular Risk Reduction: Reduces cardiovascular death and hospitalization for heart failure in patients with type 2 diabetes

• Weight Management: Mild weight loss effect due to calorie loss from urinary glucose excretion

• Emerging Indications: Research in non-alcoholic steatohepatitis (NASH), diabetic kidney disease, and other metabolic disorders

The global SGLT2 inhibitor market is expected to exceed $25 billion by 2028, driven by expanding indications in heart failure and kidney disease, growing diabetes prevalence, and increasing adoption as standard of care. Dapagliflozin continues to lead the SGLT2 class with one of the broadest indication portfolios.

Quality Specifications

Our dapagliflozin is manufactured under strict GMP conditions and meets international pharmacopeia standards:

• Purity: ≥99.0% determined by HPLC

• Identity confirmed by NMR, mass spectrometry, and infrared spectroscopy

• Water content: ≤0.5%

• Residual solvents: Meet ICH Q3C guidelines

• Heavy metals: ≤10 ppm

• Related substances: Each impurity ≤0.1%, total impurities ≤0.5%

• Enantiomeric purity: ≥99.8% ee

• Residue on ignition: ≤0.1%

• Each batch accompanied by comprehensive Certificate of Analysis (COA)

• Stable for 36 months when stored at room temperature in sealed containers

Packaging & Shipping

We offer flexible packaging options to meet diverse customer needs:

• Small quantities: 1kg, 5kg aluminum foil bags

• Bulk quantities: 25kg fiber drums with PE liners

• Custom packaging available upon request

• GMP-grade packaging available for pharmaceutical customers

• Shipped at ambient temperature

• International shipping with proper documentation

• MSDS and COA provided with each shipment