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Candesartan

Name: Candesartan
Brand: Selleck Chemicals
SKU: S1578
Rating: 5 (15 reviews)

Synonyms: CV-11974

Catalog No.S1578 Purity: 99.52%

Candesartan is an angiotensin II receptor antagonist with IC50 of 0.26 nM.

Candesartan Chemical Structure

CAS: 139481-59-7

Selleck's Candesartan has been cited by 15 Publications

1 Customer Review

Purity & Quality Control

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

99.52

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Biological Activity

Description

Candesartan is an angiotensin II receptor antagonist with IC50 of 0.26 nM.

Features

Primarily used for the treatment of hypertension.

Targets

AT1 receptor ^[1]

0.26 nM

In vitro
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. ^[1] Candesartan 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. ^[2] Candesartan (0.1 nM) could reduce the maximal contractile response to angiostensin II by approximately 50%. ^[3]
Kinase Assay	Binding assay
Kinase 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]Candesartan (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 Candesartan is added. After 30 min, 50 μL of buffer containing [³H]Candesartan (final concentration 1.1 nM) or [³H]Candesartan (final concentration 1.0 nM) is added, and the cells are further incubated for 30 min at 37 ℃.
Cell Research	Cell lines	KU-19-19 cells
	Concentrations	10 μM
	Incubation Time	48 hours
	Method	KU-19-19 cells are seeded at a cell density of 2 × 10⁴ per well in 96-well plates and allowed to grow overnight. Then the cells are treated with various concentrations of Candesartan for various periods of time. Cell viability is determined by the Alamar Blue assay to examine the cytotoxicity and antiproliferative effect of candesartan. The absorbance value of each well is determined in a microplate reade

In Vivo
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 ^[2] Candesartan (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. ^[4] Candesartan (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. ^[5]
Animal Research	Animal Models	Mouse KU-19-19 xenograft model
	Dosages	10 mg/kg
	Administration	Gavage

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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	--

References

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Chemical Information & Solubility

Molecular Weight	440.45	Formula	C₂₄H₂₀N₆O₃
CAS No.	139481-59-7	SDF	Download Candesartan SDF
Smiles	CCOC1=NC2=CC=CC(=C2N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5)C(=O)O
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 94 mg/mL ( (213.41 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 16 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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

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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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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