Irbesartan, identified by CAS NO: 138402-11-6, stands as a pivotal pharmaceutical intermediate and a highly effective active pharmaceutical ingredient (API) widely utilized in the treatment of cardiovascular conditions. This compound, primarily recognized for its role in managing hypertension, represents a significant advancement in therapeutic options for patients worldwide. Its molecular formula is C25H28N6O, with a molecular weight of 428.529, and it typically appears as a white powder, ensuring high purity for pharmaceutical applications.

At its core, Irbesartan functions as a potent and selective angiotensin II type 1 (AT1) receptor antagonist. This mechanism distinguishes it from other antihypertensive agents by specifically blocking the binding of angiotensin II to the AT1 receptor. This selective inhibition prevents the powerful vasoconstrictive effects of angiotensin II and the release of aldosterone, both of which contribute to elevated blood pressure. Importantly, Irbesartan does not interfere with the angiotensin-converting enzyme (ACE) or other hormone receptors, thereby avoiding side effects commonly associated with ACE inhibitors, such as cough, in a significant number of patients. Clinical studies have demonstrated its high affinity for the AT1 receptor, boasting an IC50 of approximately 1.3 nM, underscoring its efficacy in managing blood pressure.

The therapeutic applications of Irbesartan extend beyond mere blood pressure reduction. It is broadly prescribed for the treatment of essential hypertension, offering a reliable and sustained antihypertensive effect. Furthermore, its benefits are particularly pronounced in patients with type 2 diabetes suffering from nephropathy characterized by elevated serum creatinine and proteinuria. In these cases, Irbesartan has shown significant promise in protecting kidney function and slowing the progression of renal disease. Emerging research also indicates its potential in mitigating electrical remodeling of the myocardium, which is crucial for reducing mortality rates in hypertensive patients. Its comprehensive action makes it an indispensable component in the management of complex cardiovascular diseases.

From a pharmacokinetic perspective, Irbesartan exhibits excellent oral absorption, with a bioavailability ranging from 60% to 80%, a process that is generally unaffected by food intake. Peak plasma concentrations are typically achieved within 1 to 1.5 hours post-administration. The compound displays high plasma protein binding, usually around 90-96%, and has an elimination half-life of 11 to 15 hours, allowing for convenient once-daily dosing. Its metabolism primarily occurs through glucuronide conjugation and oxidation, predominantly mediated by the cytochrome P450 enzyme CYP2C9. Both the parent compound and its metabolites are efficiently eliminated from the body via dual pathways: biliary excretion and renal excretion, with approximately 20% of the radioactivity recovered in urine and the remainder in feces.

While generally well-tolerated, some common side effects of Irbesartan include headache, dizziness, and mild palpitation. Other reported adverse reactions, though less frequent, can involve indigestion, diarrhea, and upper respiratory tract infections. Proper storage conditions are essential to maintain its stability and efficacy: it should be stored in a well-closed container at low temperature, protected from moisture, heat, and light. Adherence to these guidelines ensures the integrity of the product over its shelf life.

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