product name Candesartan
Description: Candesartan (also known as CV-11974) is an angiotensin II receptor antagonist with IC50 of 0.26 nM. Candesartan is primarily used for the treatment of hypertension. It is marketed as the cilexetil ester, which is known as candesartan cilexetil. Candesartan cilexetil is metabolized completely by esterase in the intestinal wall during absorption to the active candesartan moiety. The use of a prodrug form increases the bioavailability of candesartan.
References: Eur J Pharmacol. 1999 Feb 19;367(2-3):413-22; Clin Cancer Res. 2006 May 1;12(9):2888-93.
440.45
Formula
C24H20N6O3
CAS No.
139481-59-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 88 mg/mL (199.8 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
30% Propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
Synonyms
CV-11974
other peoduct :
| In Vitro |
In vitro activity: Candesartan binds with high specificity to the angiotensin II AT1 receptors in CHO-AT1 cells with K−1 of 0.001 min−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. Candesartan (0.1 nM) could reduce the maximal contractile response to angiostensin II by approximately 50%. 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 Assay: 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 reader. |
|---|---|
| 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 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. 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. |
| Animal model | Mouse KU-19-19 xenograft model |
| Formulation & Dosage | Dissolved in saline; 10 mg/kg; oral gavage |
| References | Eur J Pharmacol. 1999 Feb 19;367(2-3):413-22; Clin Cancer Res. 2006 May 1;12(9):2888-93. |
