Temocapril HCl is the hydrochloride of Temocapril, which is a long-acting angiotensin-converting enzyme (ACE) inhibitor, used for the treatment of hypertension.
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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). |
| 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 |
| 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 |
| 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.
| Related ACE Products |
|---|
| Abz-Ser-Pro-3-nitro-Tyr
Abz-Ser-Pro-3-nitro-Tyr is the substrate of ACE2 (angiotensin-converting enzyme-2). |
| Temocaprilat
Temocaprilat (Temocapril diacid) is an inhibitor of angiotensin-converting enzyme (ACE). |
| FA-Phe-Phe
FA-Phe-Phe is a furylacryloyl (fa)-amino acid derivative, targeting to Angiotensin-converting Enzyme (ACE). |
| Garcinone B
Garcinone B, a xanthone derivative, is a nature product that could be isolated from the pericarp of Mangosteen. |
| Spirapril hydrochloride
Spirapril (SCH 33844) hydrochloride is a potent angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Spirapril competitively binds to ACE and prevents the conversion of angiotensin I to angiotensin II. Spirapril is an orally active proagent of Spiraprilat and can be used for the research of hypertension, congestive heart failure. |
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