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Temocapril HCl

Cat. No. M5993
Temocapril HCl Structure
Synonym:

CS-622 HCl

Size Price Availability Quantity
10mg USD 70  USD70 In stock
50mg USD 200  USD200 In stock
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Quality Control & Documentation
Biological Activity

Temocapril HCl is the hydrochloride of Temocapril, which is a long-acting angiotensin-converting enzyme (ACE) inhibitor, used for the treatment of hypertension.

Customer Product Validations & Biological Datas
Source Clin Exp Pharmacol Physiol (2012). Figure 2. Temocapril HCl
Method MMP-2 activity assay
Cell Lines
Concentrations 1 μmol/L and 10 and 100 nmol/L
Incubation Time 24 h
Results Temocaprilat inhibited MMP-2 activity in a dose-dependent manner at doses ranging from 10 nmol/L to 1 μmol/L (IC50 0.47 μmol/L).
Protocol (for reference only)
Cell Experiment
Cell lines Caco-2 cell
Preparation method For the experiments involving the transport of propranolol, naproxen and temocaprilat from the inside to the outside of cells, intact Caco-2 cell monolayers (i.e. untreated with BNPP) were used.
Concentrations 85 mM
Incubation time 5 min
Animal Experiment
Animal models Male Wistar rats
Formulation DMSO
Dosages 10–500 μM
Administration oral
Chemical Information
Molecular Weight 513.07
Formula C23H28N2O5S2.HCl
CAS Number 110221-44-8
Form Solid
Solubility (25°C) 103 mg/mL in DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Yamamoto D, et al. Clin Exp Pharmacol Physiol. Matrix metalloproteinase-2 inhibition by temocapril and its important role in peritoneal transport.

[2] Nozawa T, et al. Drug Metab Dispos. Prediction of human intestinal absorption of the prodrug temocapril by in situ single-pass perfusion using rat intestine with modified hydrolase activity.

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Keywords: Temocapril HCl, CS-622 HCl supplier, ACE, inhibitors, activators


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