| Identification | Back Directory | [Name]
Temocaprilat | [CAS]
110221-53-9 | [Synonyms]
RS-5139
Temocaprilat
Temocaprilate
Temocapril Diacid
TEMOCAPRILAT(FORR&DONLY)
[[[2S,6R]-6-[[(S)-1-Carboxy-3-phenylpropyl]amino]hexahydro-5-oxo-2-(2-thienyl)-1,4-thiazepin]-4-yl]acetic acid
(2S,6R)-6-[[(1S)-1-Carboxy-3-phenylpropyl]amino]tetrahydro-5-oxo-2-(2-thienyl)-1,4-thiazepine-4(5H)-acetic Acid
(+)-[(2S,6R)-6-[[(S)-1-(Ethoxycarbonyl)-3-phenylpropyl]amino]-5-oxo-2-(2-thienyl)perhydro-1,4-thiazepin-4-yl]acetic acid | [Molecular Formula]
C21H24N2O5S2 | [MDL Number]
MFCD00871951 | [MOL File]
110221-53-9.mol | [Molecular Weight]
448.56 |
| Chemical Properties | Back Directory | [Appearance]
White to Off-White Solid | [Melting point ]
>2300C (dec) | [alpha ]
25D +63.4° (c = 1 in DMF) | [Boiling point ]
743.6±60.0 °C(Predicted) | [density ]
1.41±0.1 g/cm3(Predicted) | [storage temp. ]
Hygroscopic, -20?C Freezer, Under Inert Atmosphere | [solubility ]
DMSO (Slightly), Methanol (Slightly) | [form ]
Solid | [pka]
2.09±0.10(Predicted) | [color ]
White to Off-White |
| Hazard Information | Back Directory | [Chemical Properties]
White to Off-White Solid | [Uses]
Antihypertensive | [Description]
Temocaprilat is an inhibitor of angiotensin-converting enzyme (ACE; IC50 = 3.6 nM for rabbit lung ACE). It inhibits contraction of isolated rat aorta induced by angiotensin I with an IC50 value of 7.6 nM. Temocaprilat (1-30 μg/kg, i.v.) inhibits angiotensin I-induced pressor responses in anesthetized rats in a dose-dependent manner. | [Definition]
ChEBI: Temocaprilat is a non-proteinogenic alpha-amino acid. | [in vivo]
Temocaprilat (1 mg/kg/d; i.v.; 4 weeks) significantly reduces systolic blood pressure with time-dependent manner in spontaneously hypertensive (SHR) rats. Temocaprilat improves myocardial fibrosis and oxidative stress in Wistar-Kyoto (WKY) rats and SHR rats[3]. | Animal Model: | Six 10-week-old WKYs and SHRs and six 50-week-old (aging control) SHRs[3]. | | Dosage: | 1 mg/kg/d. | | Administration: | Intravenous injection; 4 weeks. | | Result: | Reduced the expression levels of myocardial fibrosis, transforming growth factor-β1 (TGF-β1) mRNA and fibroblast growth factor-2 (FGF-2) mRNA in the left ventricle (LV).
Weakened the expression levels of 8-isoprostane, p22phox mRNA, p47phox mRNA and gp91phox mRNA in LV.
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| [References]
[1] KIYOSHI OIZUMI . Pharmacological Profiles of CS-622, a Novel Angiotensin Converting Enzyme Inhibitor[J]. Japanese journal of pharmacology, 1988, 48 3: Pages 349-356. DOI: 10.1254/jjp.48.349 |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
|