| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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Purity: ≥98%
Trandolapril (RU-44570; Mavik; Gopten; RU44570; Odrik), an antihypertensive drug, is an oral and nonsulfhydryl prodrug that has to be hydrolysed to the active diacid Trandolaprilat. It is a potent ACE inhibitor used to treat high blood pressure. Trandolapril acts by competitive inhibition of angiotensin converting enzyme (ACE), a key enzyme in the renin-angiotensin system which plays an important role in regulating blood pressure.
| ln Vitro |
Trandolapril (0.02 mM, 1 mM; 3 d) increases the proportion of apoptotic cells in the K562 cell line by inhibiting cell development and inducing apoptosis [2].
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| ln Vivo |
By limiting renal interstitial matrix expression and myofibroblast activation, as well as lowering renal proinflammatory cytokines RANTES and TNF-α levels in mice with renal fibrosis, trunolapril (3 mg/kg/day; oral; 7 days) decreases obstructive nephropathy in mice [2]. In rats, trundialolapril (0.3 mg/kg/day; oral; 4 weeks) reduces cellular fibronectin accumulation, collagen, and arterial hypertrophy [3]. In rats, long-term antihypertensive effects of landopril (0.3 mg/kg/day; oral; 4 months) lower blood pressure [3]. When given orally, twice daily for four months, trundialapril (0.25 mg/kg) prevents atherosclerosis in rabbits with Watanabe hereditary hyperlipidemia [4].
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| Cell Assay |
Apoptosis analysis [2]
Cell Types: K562, KU812, U937 and HL60 Tested Concentrations: 0-2 mM Incubation Duration: 0, 1, 2, 3 days Experimental Results: 1 mM inhibits K562, KU812, U937, 0.02 mM inhibits HL60. |
| Animal Protocol |
Animal/Disease Models: UUD (unilateral ureteral obstruction) model [2] in male CD-1 mice (18-22 g)
Doses: 3 mg/kg Route of Administration: po (oral gavage); one time/day for 7 days Experimental Results: Caused Renal interstitial matrix expression, including fibronectin, type I and type III collagen, is diminished and, surprisingly, myofibroblast activation is inhibited through α-smooth muscle actin (a-SMA) expression, which reduces RANTES (regulated activation, normal T cell expression and secretion) and TNF-α levels. Animal/Disease Models: SHR model (spontaneous hypertensive rats, 4 weeks old) [3] Doses: 0.3 mg/kg Route of Administration: po (oral gavage); one time/day for 4 weeks Experimental Results: The collagen content in the aortic middle layer diminished, Arterial distensibility increases by approximately 80%. Animal/Disease Models: Watanabe hereditary hyperlipidemia rabbit (3 months old) [4] Doses: 0.25 mg/kg Route of Administration: po (oral gavage); twice a day; 9-month Experimental Results: Atherosclerosis on the intimal surface Sclerosis is diminished, and the cholesterol c |
| References |
[1]. Peters DC, et al. Trandolapril. An update of its pharmacology and therapeutic use in cardiovascular disorders. Drugs. 1998 Nov;56(5):871-93.
[2]. Tan X, et al. Combination therapy with paricalcitol and trandolapril reduces renal fibrosis in obstructive nephropathy. Kidney Int. 2009 Dec;76(12):1248-57. [3]. Koffi I, et al. Prevention of arterial structural alterations with verapamil and trandolapril and consequences for mechanical properties in spontaneously hypertensive rats. Eur J Pharmacol. 1998 Nov 13;361(1):51-60. [4]. Chobanian AV, et al. Trandolapril inhibits atherosclerosis in the Watanabe heritable hyperlipidemic rabbit. Hypertension. 1992 Oct;20(4):473-7. |
| Molecular Formula |
C24H34N2O5
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|---|---|
| Molecular Weight |
430.54
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| CAS # |
87679-37-6
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| Related CAS # |
Trandolapril hydrochloride;87725-72-2;Trandolapril-d5;1356847-98-7
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| SMILES |
O=C([C@H]1N(C([C@@H](N[C@@H](CCC2=CC=CC=C2)C(OCC)=O)C)=O)[C@@]3([H])CCCC[C@]3([H])C1)O
|
| InChi Key |
VXFJYXUZANRPDJ-WTNASJBWSA-N
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| InChi Code |
InChI=1S/C24H34N2O5/c1-3-31-24(30)19(14-13-17-9-5-4-6-10-17)25-16(2)22(27)26-20-12-8-7-11-18(20)15-21(26)23(28)29/h4-6,9-10,16,18-21,25H,3,7-8,11-15H2,1-2H3,(H,28,29)/t16-,18+,19-,20-,21-/m0/s1
|
| Chemical Name |
(2S,3aR,7aS)-1-[(2S)-2-[[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino]propanoyl]-2,3,3a,4,5,6,7,7a-octahydroindole-2-carboxylic
acid
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| Synonyms |
RU 44570 Mavik RU-44570GoptenRU44570 Odrik
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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) |
DMSO : ~100 mg/mL (~232.27 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.83 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 20.8 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: ≥ 2.08 mg/mL (4.83 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.83 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3227 mL | 11.6133 mL | 23.2266 mL | |
| 5 mM | 0.4645 mL | 2.3227 mL | 4.6453 mL | |
| 10 mM | 0.2323 mL | 1.1613 mL | 2.3227 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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