Candesartan Cilexetil

SKU: orb1305541

Description

Candesartan Cilexetil is a prodrug hydrolyzed to the active AT1 receptor antagonist candesartan, which potently blocks angiotensin II-induced vasoconstriction (IC50: 0.26 nM). It is widely used in research for studying hypertension, cardiovascular remodeling, and renal function in both in vitro receptor binding assays and in vivo animal models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 145040-37-5
• MW: 610.66
• Purity: >99.99% (May vary between batches)
• Formula: C₃₃H₃₄N₆O₆
• SMILES: C(N1C=2C(N=C1OCC)=CC=CC2C(OC(OC(OC3CCCCC3)=O)C)=O)C4=CC=C(C=C4)C5=C(C=CC=C5)C=6NN=NN6
• Target: Apoptosis,RAAS
• Solubility: DMSO:250 mg/mL (409.39 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.28 mM)

Bioactivity

• Target IC50:
  Ang II receptor:0.26 nM
• In Vivo:
  The prodrug of Candesartan is absorbed through the gastrointestinal tract and activated by ester hydrolysis into Candesartan. Candesartan then blocks the effects of angiotensin II on the angiotensin II type 1 receptors.
• In Vitro:
  Five hours post-administration, Candesartan (1 mg/kg, orally) reduced blood pressure to a similar extent as Enalapril (10 mg/kg, orally) on both the 1st and 7th days. Candesartan significantly increased renal blood flow without altering the cardiac index. In rat myocardium with dilated cardiomyopathy (DCM), Candesartan dose-dependently improved functional markers and upregulated angiotensin (1-7), ACE2, and MAS1. Treatment with Candesartan in rats led to a reduction in various endoplasmic reticulum (ER) stress markers, apoptotic markers, and the number of apoptotic cells. Furthermore, Candesartan demonstrated a dose-dependent blockade of angiotensin-II in rats with dilated cardiomyopathy.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Candesartan Cilexetil, Apoptosis, Angiotensin Receptor, angiotensin II receptor, Inhibitor, inhibit, TCV 116, TCV116, TCV-116

Compound Identifiers

PubChem CID

2540