Temocapril hydrochloride

Cat. No.: HY-B0384 Purity: 99.83%: FAQs
Data Sheet SDS COA Handling Instructions

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Temocapril hydrochloride is an orally active angiotensin-converting enzyme (ACE) inhibitor. Temocapril hydrochloride 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 hydrochloride Chemical Structure

CAS No. : 110221-44-8

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 43	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 43	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 38	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 115	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 280	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Other Forms of Temocapril hydrochloride:

Temocapril-d₅ Get quote
Temocapril Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

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 on neurogenic vasodilation in the SHR^[2].
Temocapril hydrochloride (0.1-10 μM; 24 h) shows inductive effects on redox proteins 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.

Cell Proliferation Assay^[3]

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

In Vivo

Temocapril hydrochloride (10 mg/kg; p.o.; 21 d) enhances cardiomyocyte thioredoxin expression and ameliorates autoimmune myocarditis^[3].
Temocapril hydrochloride (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^[1]
Dosage:	30 mg/kg
Administration:	Oral administration, daily, for 4 weeks
Result:	Suppressed the blood pressure elevation induced by Ang I.

Molecular Weight

513.07

Formula

C₂₃H₂₉ClN₂O₅S₂

CAS No.

110221-44-8

Appearance

Solid

Color

White to off-white

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.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 62.5 mg/mL (121.82 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 2.27 mg/mL (4.42 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	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

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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 2.08 mg/mL (4.05 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.05 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.05 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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 (sealed storage, away from moisture)

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: 99.83%

Select Batch:

Data Sheet (282 KB) SDS (393 KB)

COA (255 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

References

[1]. Fukami T, et al. In vitro evaluation of inhibitory effects of antidiabetic and antihyperlipidemic drugs on human carboxylesterase activities. Drug Metab Dispos. 2010 Dec;38(12):2173-8. [Content Brief]

[2]. Kawasaki H, et al. Angiotensin inhibits neurotransmission of calcitonin gene-related peptide-containing vasodilator nerves in mesenteric artery of spontaneously hypertensive rats. J Pharmacol Exp Ther. 1998 Feb;284(2):508-15. [Content Brief]

[3]. Yuan Z, et al. Temocapril treatment ameliorates autoimmune myocarditis associated with enhanced cardiomyocyte thioredoxin expression. Cardiovasc Res. 2002 Aug 1;55(2):320-8. [Content Brief]

[4]. Ohnishi K, et al. Angiotensin-converting enzyme inhibitor does not suppress renal angiotensin II levels in angiotensin I-infused rats. J Pharmacol Sci. 2013;122(2):103-8. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	1.9491 mL	9.7453 mL	19.4905 mL	48.7263 mL
DMSO	5 mM	0.3898 mL	1.9491 mL	3.8981 mL	9.7453 mL
	10 mM	0.1949 mL	0.9745 mL	1.9491 mL	4.8726 mL
	15 mM	0.1299 mL	0.6497 mL	1.2994 mL	3.2484 mL
	20 mM	0.0975 mL	0.4873 mL	0.9745 mL	2.4363 mL
	25 mM	0.0780 mL	0.3898 mL	0.7796 mL	1.9491 mL
	30 mM	0.0650 mL	0.3248 mL	0.6497 mL	1.6242 mL
	40 mM	0.0487 mL	0.2436 mL	0.4873 mL	1.2182 mL
	50 mM	0.0390 mL	0.1949 mL	0.3898 mL	0.9745 mL
	60 mM	0.0325 mL	0.1624 mL	0.3248 mL	0.8121 mL
	80 mM	0.0244 mL	0.1218 mL	0.2436 mL	0.6091 mL
	100 mM	0.0195 mL	0.0975 mL	0.1949 mL	0.4873 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.