Trandolapril (RU44570) HCl is a non-sulfhydryl precursor compound that hydrolyzes to active diacetyl (Trandolapril HClat). Trandolapril HCl is an orally bioactive angiotensin-converting enzyme (ACE) inhibitor utilized in the research of hypertension and congestive heart failure (CHF) and myocardial infarction (MI).

Physicochemical Properties

Molecular Formula	C24H35CLN2O5
Molecular Weight	467.00
Exact Mass	466.223
CAS #	87725-72-2
Related CAS #	Trandolapril;87679-37-6
PubChem CID	67422545
Appearance	Typically exists as solid at room temperature
LogP	3.904
Hydrogen Bond Donor Count	3
Hydrogen Bond Acceptor Count	6
Rotatable Bond Count	10
Heavy Atom Count	32
Complexity	634
Defined Atom Stereocenter Count	5
SMILES	Cl.C[C@@H](C(N1[C@H](C(=O)O)C[C@@H]2[C@@H]1CCCC2)=O)N[C@H](C(OCC)=O)CCC1=CC=CC=C1
InChi Key	QNSWMJYOGMUVGO-REWXTUPXSA-N
InChi Code	InChI=1S/C24H34N2O5.ClH/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);1H/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;hydrochloride
HS Tariff Code	2934.99.9001
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)

Biological Activity

Targets	Target: Angiotensin-converting Enzyme (ACE)[1]
ln Vivo	In mice with obstructive nephropathy, tandolapril hydrochloride (3 mg/kg/day; po; 7 d) reduces renal fibrosis by blocking the expression of the renal interstitial matrix and myofibroblast activation, which in turn lowers renal proinflammatory cytokine RANTES and TNF-α levels[2]. (0.3 mg/kg/day; po; 4 weeks) inhibits the buildup of collagen and cellular fibronectin, arterial hypertrophy, and enhances arterial mechanics in rats[3]. In rats, randolapril (0.3 mg/kg/day; po; 4 months) has long-term anti-hypertensive effects that lower blood pressure[3]. In the Watanabe Heritable Hyperlipidemic Rabbit, trandolapril hydrochloride (0.25 mg/kg; po; twice a day; 4 months) prevents atherosclerosis[4].
Animal Protocol	Animal/Disease Models: UUD (unilateral ureteral obstruction) model in Male CD-1 mice (18-22 g)[2] Doses: 3 mg/kg Route of Administration: Oral gavage; daily, for 7 days Experimental Results: Resulted in renal interstitial matrix expression (including fibronectin, type I, and type III collagen) decreasing, and inhibited myofibroblast activation by surprising a-smooth muscle actin (a-SMA) expression, diminished the RANTES (regulated on activation, normal T cell expressed and secreted) and TNF-α level. Animal/Disease Models: SHR model (spontaneously hypertensive rats, 4weeks old)[3] Doses: 0.3 mg/kg Route of Administration: Oral gavage; daily for 4 weeks Experimental Results: decreased collagen content in the aortic media and increased ariterial distensibility up to about 80%. Animal/Disease Models: Watanabe heritable hyperlipidemic rabbit (3 months old)[4] Doses: 0.25 mg/kg Route of Administration: Oral gavage; twice a day; 9 months Experimental Results: diminished in atherosclerotic involvement of the intimal surface, and also diminished cholesterol content in descending thoracic ao
References	[1]. Trandolapril. An update of its pharmacology and therapeutic use in cardiovascular disorders. Drugs. 1998 Nov;56(5):871-93. [2]. Combination therapy with paricalcitol and trandolapril reduces renal fibrosis in obstructive nephropathy. Kidney Int. 2009 Dec;76(12):1248-57. [3]. 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]. Trandolapril inhibits atherosclerosis in the Watanabe heritable hyperlipidemic rabbit. Hypertension. 1992 Oct;20(4):473-7.

Solubility Data

Solubility (In Vitro)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Solubility (In Vivo)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples. Injection Formulations (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] *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. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.1413 mL	10.7066 mL	21.4133 mL
	5 mM	0.4283 mL	2.1413 mL	4.2827 mL
	10 mM	0.2141 mL	1.0707 mL	2.1413 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.