100277-62-1
Chemical Structure
CV 5975
- CAS No.: 100277-62-1
- Formula:C22H31N3O5S
- Molecular Weight:449.56
InChIKey: VGLXNWGVKZBOQS-IRXDYDNUSA-N
SMILES: OC(CN1C2=CC=CC=C2SC[C@@H](C1=O)N[C@H](C(O)=O)CCCCC3CCNCC3)=O
Biological Activity: CV 5975 is an orally active angiotensin converting enzyme (ACE) competitive inhibitor with a rabbit lung ACE IC50 of 3.1 nM and Ki values of 2.6 nM. CV 5975 inhibits ACE in plasma, aorta, kidney, and brain, intensifying inhibition with repeated administration. CV 5975 inhibits Angiotensin I (HY-P1032)-induced pressor responses and ileum contraction, and augments bradykinin-induced ileum contraction and depressor responses. CV 5975 reduces blood pressure via ACE-independent mechanisms, with sustained action across multiple hypertensive and normotensive animal models, intensified by repeated dosing or Hydrochlorothiazide (HY-B0252) co-administration. CV 5975 can be used for the research of hypertension[1][2][3][4].
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CV 5975 | CV 5975 is an orally active angiotensin converting enzyme (ACE) competitive inhibitor with a rabbit lung ACE IC50 of 3.1 nM and Ki values of 2.6 nM. CV 5975 inhibits ACE in plasma, aorta, kidney, and brain, intensifying inhibition with repeated administration. CV 5975 inhibits Angiotensin I (HY-P1032)-induced pressor responses and ileum contraction, and augments bradykinin-induced ileum contraction and depressor responses. CV 5975 reduces blood pressure via ACE-independent mechanisms, with sustained action across multiple hypertensive and normotensive animal models, intensified by repeated dosing or Hydrochlorothiazide (HY-B0252) co-administration. CV 5975 can be used for the research of hypertension. | |||||||||||||||||||||
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- [1]. Kori M, et al. An improved synthesis of the new angiotensin converting enzyme inhibitor CV-5975 via a chemoenzymatic process. Chem Pharm Bull (Tokyo). 1987 Jun;35(6):2319-26. [Content Brief]
- [2]. Inada Y, et al. (R)-3-[(S)-1-carboxy-5-(4-piperidyl)pentyl]amino-4-oxo-2,3,4,5- tetrahydro-1,5-benzothiazepine-5-acetic acid (CV-5975): a new potent and long-lasting inhibitor of angiotensin converting enzyme. Jpn J Pharmacol. 1988;47(2):135-141. [Content Brief]
- [3]. Inada Y, et al. Antihypertensive action of a new angiotensin converting enzyme inhibitor, (R)-3-[(S)-1-carboxy-5-(4-piperidyl)pentyl]amino-4-oxo-2,3,4,5-tetr ahy dro-1,5-benzothiazepine-5-acetic acid (CV-5975), in various hypertensive models. Jpn J Pharmacol. 1988;47(3):311-322. [Content Brief]
- [4]. Inada Y, et al. Inhibition of angiotensin converting enzyme by (R)-3-[(S)-1-carboxy-5-(4-piperidyl)pentyl]amino-4-oxo-2,3,4,5-tetra- hydro-1,5-benzothiazepine-6-acetic acid (CV-5975), a non-sulfhydryl compound. Jpn J Pharmacol. 1988;48(3):323-330. [Content Brief]
Keywords
