1. Metabolic Enzyme/Protease
  2. Angiotensin-converting Enzyme (ACE)
  3. Temocapril

Temocapril is an orally active angiotensin-converting enzyme (ACE) inhibitor. Temocapril can be used for the research of hypertension, congestive heart failure, acute myocardial infarction, insulin resistance, and renal diseases.

For research use only. We do not sell to patients.

Temocapril Chemical Structure

Temocapril Chemical Structure

CAS No. : 111902-57-9

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Temocapril:

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  • Biological Activity

  • Purity & Documentation

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Description

Temocapril is an orally active angiotensin-converting enzyme (ACE) inhibitor. Temocapril can be used for the research of hypertension, congestive heart failure, acute myocardial infarction, insulin resistance, and renal diseases[1][2].

IC50 & Target

Angiotensin-converting Enzyme (ACE)[1]

In Vitro

Temocapril hydrochloride is a prodrug of the ACE inhibitor, Temocaprilat. Temocapril hydrochloride can be readily uptaken via the small intestine, and then be converted to its active metabolite (temocaprilat) by CES1 (human carboxylesterase 1) in the liver[1].
Temocapril hydrochloride (500 nM) reduces the inhibitory effects of RS (N-acetyltetradecapeptide renin substrate) and AngI (angiotensin) on neurogenic vasodilation in the spontaneously hypertensive rats (SHR)[2].
Temocapril hydrochloride (0.1-10 μM; 24 h) shows inductive effects on redox proteins thioredoxin (TRX) while no effect on antioxidant enzymes Cu/ZnSOD and Mn-SOD expressions[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[3]

Cell Line: Cultured neonatal rat cardiomyocytes
Concentration: 0.1 μM, 1 μM, 10 μM
Incubation Time: 24 hours
Result: Enhanced redox proteins thioredoxin (TRX) expression 1.9-fold at 10 μM without affecting TRX2, Cu/Zn-SOD or Mn-SOD protein expression.
In Vivo

Temocapril (10 mg/kg; p.o.; 21 d) enhances cardiomyocyte thioredoxin expression and ameliorates autoimmune myocarditis[3].
Temocapril (30 mg/kg; p.o.; daily; for 4 weeks) suppresses Angiotensin I-induced hypertension, plasma and renal ACE activity, but fails to reduce the level of Ang II in the kidney[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Experimental autoimmune myocarditis (EAM) rat model[3]
Dosage: 10 mg/kg
Administration: Oral gavage; administration by water; 21 days
Result: Ameliorated EAM and prevented cellular proteins from oxidation.
Enhanced cardiomyocyte redox regulatory protein TRX expression.
Animal Model: Male Sprague Dawley rats[4]
Dosage: 30 mg/kg
Administration: Oral gavage, daily, for 4 weeks
Result: Suppressed the blood pressure elevation induced by Ang I.
Molecular Weight

476.61

Formula

C23H28N2O5S2

CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C(O)CN1C[C@@H](C2=CC=CS2)SC[C@H](N[C@H](C(OCC)=O)CCC3=CC=CC=C3)C1=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (209.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0982 mL 10.4908 mL 20.9815 mL
5 mM 0.4196 mL 2.0982 mL 4.1963 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.25 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.25 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.14%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0982 mL 10.4908 mL 20.9815 mL 52.4538 mL
5 mM 0.4196 mL 2.0982 mL 4.1963 mL 10.4908 mL
10 mM 0.2098 mL 1.0491 mL 2.0982 mL 5.2454 mL
15 mM 0.1399 mL 0.6994 mL 1.3988 mL 3.4969 mL
20 mM 0.1049 mL 0.5245 mL 1.0491 mL 2.6227 mL
25 mM 0.0839 mL 0.4196 mL 0.8393 mL 2.0982 mL
30 mM 0.0699 mL 0.3497 mL 0.6994 mL 1.7485 mL
40 mM 0.0525 mL 0.2623 mL 0.5245 mL 1.3113 mL
50 mM 0.0420 mL 0.2098 mL 0.4196 mL 1.0491 mL
60 mM 0.0350 mL 0.1748 mL 0.3497 mL 0.8742 mL
80 mM 0.0262 mL 0.1311 mL 0.2623 mL 0.6557 mL
100 mM 0.0210 mL 0.1049 mL 0.2098 mL 0.5245 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Temocapril
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