Home GPCR & G Protein Angiotensin Receptor antagonist Candesartan

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Candesartan Angiotensin Receptor antagonist

Cat.No.S1578

Candesartan is an angiotensin II receptor antagonist with IC50 of 0.26 nM.
Candesartan Angiotensin Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 440.45

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Quality Control

Batch: S157802 DMSO]94 mg/mL]false]Ethanol]16 mg/mL]false]Water]Insoluble]false Purity: 99.52%
99.52

Solubility

In vitro
Batch:

DMSO : 94 mg/mL (213.41 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 16 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 440.45 Formula

C24H20N6O3

 Storage (From the date of receipt)
CAS No. 139481-59-7 Download SDF Storage of Stock Solutions

Synonyms CV-11974 SMILES CCOC1=NC2=CC=CC(=C2N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5)C(=O)O

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Mechanism of Action

Features
Primarily used for the treatment of hypertension.
Targets/IC50/Ki
AT1 receptor
0.26 nM
In vitro
Candesartan binds with high specificity to the angiotensin II AT1 receptors in CHO-AT1 cells with K−1 of 0.001 min−1. This compound does not affect cell viability or proliferation but increases the expression of VEGF and interleukin-8 in the cultured medium of KU-19-19 cells. It (0.1 nM) could reduce the maximal contractile response to angiostensin II by approximately 50%.
Kinase Assay
Binding assay
Cells are plated in 24-well plates and cultured until confluence. Before the experiment, the cells are washed three times with 0.5 mL per well of DMEM at room temperature. After removal of the medium, 400 μL binding DMEM is added and the plate is then left for 15 min at 37 ℃. For saturation binding assays cells are incubated with increasing concentrations [3H]this compound (final concentrations between 0.15 nM and 15 nM) in a final volume of 0.5 mL at 37 ℃ for 5 min to 180 min. For competition binding assays 50 μL of buffer or 50 μL of buffer containing increasing concentrations of unlabelled this chemical is added. After 30 min, 50 μL of buffer containing [3H]this compound (final concentration 1.1 nM) or [3H]this chemical (final concentration 1.0 nM) is added, and the cells are further incubated for 30 min at 37 ℃.
In vivo
Candesartan (10 mg/kg) inhibits the growth of engrafted tumors and reduces the microvessel density and VEGF expression in a mouse KU-19-19 xenograft model This compound (0.5 mg/kg) decreases blood pressure and inhibits AT1 binding in the subfornical organ (SFO), paraventricular nucleus of the hypothalamus (PVN), nucleus of the solitary tract (NTS) and area postrema (AP) in WKY rats. This chemical (0.3 mg/kg) pretreatment decreases the infarct area by 31% in adult spontaneously hypertensive rats, reduces the CBF decrease at the peripheral area of ischemia and the cortical volume of severe ischemic lesion.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/10882779/
  • [5] https://pubmed.ncbi.nlm.nih.gov/12215602/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-06-17)

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