Candesartan cilexetilCAS# 145040-37-5 |
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| Cas No. | 145040-37-5 | SDF | Download SDF |
| PubChem ID | 2540 | Appearance | Powder |
| Formula | C33H34N6O6 | M.Wt | 610.7 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | TCV-116 | ||
| Solubility | DMSO : ≥ 50 mg/mL (81.88 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 1-cyclohexyloxycarbonyloxyethyl 2-ethoxy-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]benzimidazole-4-carboxylate | ||
| SMILES | CCOC1=NC2=CC=CC(=C2N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5)C(=O)OC(C)OC(=O)OC6CCCCC6 | ||
| Standard InChIKey | GHOSNRCGJFBJIB-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C33H34N6O6/c1-3-42-32-34-28-15-9-14-27(31(40)43-21(2)44-33(41)45-24-10-5-4-6-11-24)29(28)39(32)20-22-16-18-23(19-17-22)25-12-7-8-13-26(25)30-35-37-38-36-30/h7-9,12-19,21,24H,3-6,10-11,20H2,1-2H3,(H,35,36,37,38) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Prodrug of the angiotensin II receptor 1 (AT1) antagonist candesartan (Cat. No. 4791), which exhibits antihypertensive effects in animal models. |
Candesartan cilexetil Dilution Calculator
Candesartan cilexetil Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.6375 mL | 8.1873 mL | 16.3747 mL | 32.7493 mL | 40.9366 mL |
| 5 mM | 0.3275 mL | 1.6375 mL | 3.2749 mL | 6.5499 mL | 8.1873 mL |
| 10 mM | 0.1637 mL | 0.8187 mL | 1.6375 mL | 3.2749 mL | 4.0937 mL |
| 50 mM | 0.0327 mL | 0.1637 mL | 0.3275 mL | 0.655 mL | 0.8187 mL |
| 100 mM | 0.0164 mL | 0.0819 mL | 0.1637 mL | 0.3275 mL | 0.4094 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Candesartan Cilexetil (TCV-116) is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. Target: Type-1 angiotensin II receptor Candesartan is generally well tolerated and significantly reduced cardiovascular deaths and hospital admissions for heart failure. Ejection fraction or treatment at baseline did not alter these effects [1]. In rats, TCV-116 inhibited the pressor responses to Ang I, Ang II, and Ang III without an effect on the bradykinin (BK)-induced depressor response. In SHR, the antihypertensive effect of TCV-116 (10 mg/kg) was larger than the maximum antihypertensive effect of enalapril and was not intensified by combination with enalapril. TCV-116 is more effective than enalapril in reducing blood pressure in SHR and 1K, 1C-HR, and that the BK- and/or prostaglandin-potentiating effect of enalapril contributes little to its antihypertensive mechanism in SHR [2].
References:
[1]. Pfeffer, M.A., et al., Effects of candesartan on mortality and morbidity in patients with chronic heart failure: the CHARM-Overall programme. Lancet, 2003. 362(9386): p. 759-66.
[2]. Wada, T., et al., Comparison of the antihypertensive effects of the new angiotensin II (AT1) receptor antagonist candesartan cilexetil (TCV-116) and the angiotensin converting enzyme inhibitor enalapril in rats. Hypertens Res, 1996. 19(2): p. 75-81.
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Three dimensional macroporous hydroxyapatite/chitosan foam-supported polymer micelles for enhanced oral delivery of poorly soluble drugs.[Pubmed:29960950]
Colloids Surf B Biointerfaces. 2018 Oct 1;170:497-504.
In the current study, a novel three-dimensional macroporous hydroxyapatite/ chitosan foam (HA/CS)-supported polymer micelle (PM/HA/CS) was developed, and its potential as an oral drug delivery system to enhance the solubility and oral bioavailability of poorly soluble compounds was systemically studied. Candesartan cilexetil (CC) was selected as a poorly soluble model drug. Firstly, HA/CS foam was synthesized using a wet chemical co-precipitation approach and poly-(methyl methacrylate) colloidal crystals as a macropore template. Subsequently, the CC-loaded polymer micelles were efficiently encapsulated into the macropores of the HA/CS foam and freeze-dried to produce powdery CC-loaded PM/HA/CS composites (CC-PM/HA/CS). The resulting CC-PM/HA/CS particles were then characterized in terms of porous structure, morphology, angle of repose, crystallinity, drug loading, dissolution profiles, and physical stability. Differential scanning calorimetry (DSC) analysis confirmed that CC-PM/HA/CS was present in an amorphous form and has an excellent physical stability. Under both simulated gastric and intestinal conditions, the aqueous solubility and dissolution rate of the PM/HA/CS-based CC formulation were significantly increased compared with the pure drug powder. In addition, PM/HA/CS is almost completely non-cytotoxic. The PM/HA/CS-based CC formulation produced approximately 1.9-fold increased bioavailability when compared to the marketed tablets (Blopress((R))) administered to fasted Sprague-Dawley rats. On the whole, PM/HA/CS benefits from the advantages of three dimensional macroporous HA/CS foam and polymer micelles, and exhibits great potential as a drug delivery system for increasing the solubility and oral bioavailability of a poorly soluble compound, like CC.
