Temocapril HCl

Alias: CS-622 HCl;CS-622;CS 622;CS622;Temocaprilum
Cat No.:V1791 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 HCl Chemical Structure CAS No.: 110221-44-8
Product category: RAAS
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
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Other Forms of Temocapril HCl:

  • Temocapril
  • Temocapril-d5 (Temocapril-d5)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

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.

Biological Activity I Assay Protocols (From Reference)
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].
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].
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.
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.
[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.
[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.
[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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C23H28N2O5S2.HCL
Molecular Weight
513.07
CAS #
110221-44-8
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
Synonyms
CS-622 HCl;CS-622;CS 622;CS622;Temocaprilum
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)
Solubility Data
Solubility (In Vitro)
DMSO: 103 mg/mL (200.8 mM)
Water:<1 mg/mL
Ethanol:103 mg/mL (200.8 mM)
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.

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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.
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Biological Data
  • Temocapril HCl

  • Temocapril HCl

  • Temocapril HCl

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