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Purity: ≥98%
Candesartan (also known as CV-11974; Blopress, Atacand, Amias, Ratacand) is an approved antihypertensive drug acting as an AT II/angiotensin II receptor antagonist with IC50 of 0.26 nM. Candesartan is primarily used for the treatment of hypertension. It is marketed as the prodrug form: 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.
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| ln Vivo |
In lowering neuronal damage, lesion volume, and microglial activation, candesartan (ip; 1 mg/kg/day; for 1, 3, or 28 dpi) is neuroprotective, protecting CBF, and improving TBI animal models. Operational conduct [3].
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| Animal Protocol |
Animal/Disease Models: C57BL/6 mice (nineweeks old, male, 22–28 g)[3]
Doses: 1 mg/kg Route of Administration: ip; 1 mg/kg/day; continuously for 1, 3 or 28 dpi. Experimental Results: decreased the lesion volume after CCI injury by approximately 50%, diminished the number of dying neurons, lessened the number of activated microglial cells, protected cerebral blood flow (CBF), and decreased the expression of the cytokine TGFß1 while increasing expression of TGFB3 . demonstrated good motor skills on the rotarod 3 days after injury, and improved performance in the Morris water maze 4 weeks after injury. |
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| References |
[1]. Pfeffer MA, et al. Effects of candesartan on mortality and morbidity in patients with chronic heart failure: the CHARM-Overall programme. Lancet. 2003 Sep 6;362(9386):759-66.
[2]. Nishimura Y, et al. Chronic peripheral administration of the angiotensin II AT(1) receptor antagonist candesartan blocks brain AT(1) receptors. Brain Res. 2000 Jul 14;871(1):29-38. [3]. Sonia Villapol, et al. Candesartan, an angiotensin II AT₁-receptor blocker and PPAR-γ agonist, reduces lesion volume and improves motor and memory function after traumatic brain injury in mice. Neuropsychopharmacology. 2012 Dec;37(13):2817-29. |
| Molecular Formula |
C24H20N6O3
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|---|---|
| Molecular Weight |
440.45
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| CAS # |
139481-59-7
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| Related CAS # |
Candesartan Cilexetil;145040-37-5;Candesartan-d4;1346604-70-3;Candesartan-d5;1189650-58-5
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| SMILES |
O(C([H])([H])C([H])([H])[H])C1=NC2=C([H])C([H])=C([H])C(C(=O)O[H])=C2N1C([H])([H])C1C([H])=C([H])C(C2=C([H])C([H])=C([H])C([H])=C2C2N=NN([H])N=2)=C([H])C=1[H]
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| Synonyms |
CV11974; CV-11974, CV 11974, Trade names: Blopress, Atacand, Amias, and Ratacand
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.68 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.68 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 30%Propylene glycol, 5%Tween 80, 65% D5W:30 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2704 mL | 11.3520 mL | 22.7041 mL | |
| 5 mM | 0.4541 mL | 2.2704 mL | 4.5408 mL | |
| 10 mM | 0.2270 mL | 1.1352 mL | 2.2704 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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