Home GPCR & G Protein Angiotensin Receptor antagonist Candesartan

research use only

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

Jump to

Quality Control

Batch: S157802 DMSO]94 mg/mL]false]Ethanol]16 mg/mL]false]Water]Insoluble]false Purity: 99.52%
  • Cited in Nature Medicine for its top-tier quality
  • COA
  • NMR
  • HPLC
  • SDS
  • Datasheet
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

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg
g
μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO
%
% Tween 80
% ddH2O
% DMSO
+
%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

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 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05321875 Recruiting
Cardiomyopathy Dilated
Cristina Avendaño Solá|Puerta de Hierro University Hospital
 June 2 2022 Phase 3
NCT04012307 Completed
Bioequivalence
Pharmtechnology LLC|Altasciences Company Inc.
 July 11 2019 Phase 1
NCT03017950 Completed
Hypertension|Hyperlipidemias
Chong Kun Dang Pharmaceutical
 December 2016 Phase 1
NCT03460327 Recruiting
Obesity Morbid
Norwegian University of Science and Technology|St. Olavs Hospital|Volvat Medisinsk Senter Stokkan|Namsos Hospital|Alesund Hospital
 November 2 2016 --

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.