| 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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| 500mg |
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| Other Sizes |
Purity: ≥98%
Temocapril HCl is the hydrochloride of Temocapril, which is a long-acting angiotensin-converting enzyme (ACE) inhibitor, it is used for the treatment of hypertension. Temocapril is a prodrug-type ACE inhibitor not approved for use in the United States, but is approved in Japan and South Korea. Temocapril can also be used in hemodialysis patients without risk of serious accumulation.
| Targets |
Angiotensin-converting enzyme (ACE); [3]
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| ln Vitro |
The prodrug of Temocaprilat, an ACE inhibitor, is Temocapril hydrochloride. Temoprilat hydrochloride is easily absorbed by the small intestine and then processed by CES1 (human carboxylesterase 1) in the liver to produce its active metabolite, temoprilat [1]. The inhibitory effects of AngI and RS (N-acetyl tetradecapeptide renin substrate) on SHR neurogenic vasodilation are lessened by temocapril hydrochloride (500 nM) [2]. Temocapril hydrochloride (0.1–10 μM; 24 h) induces the redox protein TRX, but does not change the production of Mn-SOD and Cu/ZnSOD, two antioxidant enzymes [3].
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| ln Vivo |
Improved thioredoxin expression in cardiomyocytes and amelioration of autoimmune myocarditis are two benefits of temopril hydrochloride (10 mg/kg; oral; 21 days) [3]. For four weeks, temopril hydrochloride (30 mg/kg; oral; daily) reduces renal ACE activity, plasma, and angiotensin I-induced hypertension, but not renal Ang II levels [4].
In a Lewis rat model of autoimmune myocarditis induced by porcine cardiac myosin (emulsified in complete Freund's adjuvant, immunized on day 0), oral administration of Temocapril HCl (10 mg/kg/day, dissolved in drinking water) from day 0 to day 21 post-immunization significantly ameliorated myocardial inflammation. Specific results included: 1. Myocardial mononuclear cell infiltration was reduced by 58% ± 6% compared to the model group (assessed by histological staining). 2. The area of myocardial necrosis decreased from 22% ± 3% (model group) to 8% ± 2% (Temocapril group). 3. Myocardial inflammation scores (scored 0–4 based on histological severity) decreased from 3.1 ± 0.3 to 1.2 ± 0.2. 4. Western blot and immunohistochemical staining showed that the expression level of thioredoxin (a redox-regulating protein) in cardiomyocytes was upregulated by 2.3-fold ± 0.2-fold compared to the model group [3] |
| Cell Assay |
Cell proliferation assay [3]
Cell Types: cultured neonatal rat cardiomyocytes Tested Concentrations: 0.1 μM, 1 μM, 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: TRX protein expression was enhanced 1.9 times at 10 μM without affecting TRX2 and Cu/Zn -SOD or Mn-SOD protein expression. |
| Animal Protocol |
Animal/Disease Models: Experimental autoimmune myocarditis (EAM) rat model [3]
Doses: 10 mg/kg Route of Administration: po (oral gavage); water management; 21-day Experimental Results: Improve EAM and prevent cellular protein oxidation. The expression of redox regulatory protein TRX in cardiomyocytes is enhanced. Animal/Disease Models: Male Sprague Dawley rats [1] Doses: 30 mg/kg Route of Administration: Orally, one time/day for 4 weeks Experimental Results: Inhibition of Ang I-induced increase in blood pressure. Establishment of autoimmune myocarditis model in Lewis rats: 1. Animal grouping: Male Lewis rats (6–8 weeks old, 180–220 g) were randomly divided into two groups (n=8 per group): - Model group: Immunized with porcine cardiac myosin (2 mg/mL, emulsified with equal volume of complete Freund's adjuvant) via subcutaneous injection (0.2 mL per rat) on day 0, and given plain drinking water for 21 days. - Temocapril HCl treatment group: Immunized with porcine cardiac myosin (same as model group) on day 0, and given drinking water containing Temocapril HCl (adjusted to a dosage of 10 mg/kg/day based on daily water intake) for 21 days. 2. Sample collection: On day 21 post-immunization, all rats were euthanized by carbon dioxide inhalation. The hearts were quickly excised, rinsed with normal saline, and divided into two parts: one part was fixed in 4% paraformaldehyde for histological analysis (HE staining) and immunohistochemical staining (thioredoxin detection); the other part was stored at -80°C for Western blot analysis (thioredoxin protein expression detection) [3] |
| References |
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| Additional Infomation |
Temocapril hydrochloride is a dipeptide. Temopril hydrochloride is an angiotensin-converting enzyme inhibitor (ACEI), and its pharmacological effect is to reduce the conversion of angiotensin I to angiotensin II (a potent vasoconstrictor) by inhibiting ACE. In an autoimmune myocarditis model, the ameliorative effect of temopril hydrochloride is closely related to the enhanced expression of thioredoxin in cardiomyocytes: thioredoxin can scavenge intracellular reactive oxygen species (ROS), inhibit cardiomyocyte apoptosis, and reduce the secretion of inflammatory cytokines (such as TNF-α and IL-6), thereby protecting myocardial tissue from immune-mediated damage [3].
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| Molecular Formula |
C23H28N2O5S2.HCL
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| Molecular Weight |
513.07
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| Exact Mass |
512.12
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| CAS # |
110221-44-8
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| Related CAS # |
Temocapril;111902-57-9;Temocapril-d5;1356840-03-3
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| PubChem CID |
443873
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| Appearance |
White to off-white solid powder
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| Boiling Point |
717.4ºC at 760 mmHg
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| Melting Point |
196-200ºC (dec)
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| Flash Point |
387.7ºC
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| Vapour Pressure |
1.34E-21mmHg at 25°C
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| Index of Refraction |
1.628
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| LogP |
1.284
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
33
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| Complexity |
644
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CCOC(=O)[C@H](CCC1=CC=CC=C1)N[C@H]2CS[C@@H](CN(C2=O)CC(=O)O)C3=CC=CS3.Cl
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| InChi Key |
XDDQNOKKZKHBIX-ASBZXGSUSA-N
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| InChi Code |
InChI=1S/C23H28N2O5S2.ClH/c1-2-30-23(29)17(11-10-16-7-4-3-5-8-16)24-18-15-32-20(19-9-6-12-31-19)13-25(22(18)28)14-21(26)27;/h3-9,12,17-18,20,24H,2,10-11,13-15H2,1H3,(H,26,27);1H/t17-,18-,20-;/m0./s1
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| Chemical Name |
2-[(2S,6R)-6-[[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino]-5-oxo-2-thiophen-2-yl-1,4-thiazepan-4-yl]acetic acid;hydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| 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: ≥ 2.08 mg/mL (4.05 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 (4.05 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 (4.05 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 | 1.9491 mL | 9.7453 mL | 19.4905 mL | |
| 5 mM | 0.3898 mL | 1.9491 mL | 3.8981 mL | |
| 10 mM | 0.1949 mL | 0.9745 mL | 1.9491 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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