| Identification | Back Directory | [Name]
Remikiren | [CAS]
126222-34-2 | [Synonyms]
C07465
D09038
AC1O44IV
Remikiren
Ro-42-5892
CHEMBL31601
(αS)-α-[[(S)-2-(tert-Butylsulfonylmethyl)-1-oxo-3-phenylpropyl]amino]-N-[(1S,2R,3S)-1-(cyclohexylmethyl)-3-cyclopropyl-2,3-dihydroxypropyl]-1H-imidazole-4-propanamide
1H-Imidazole-5-propanamide, N-[(1S,2R,3S)-1-(cyclohexylmethyl)-3-cyclopropyl-2,3-dihydroxypropyl]-α-[[(2S)-2-[[(1,1-dimethylethyl)sulfonyl]methyl]-1-oxo-3-phenylpropyl]amino]-, (αS)- | [Molecular Formula]
C33H50N4O6S | [MDL Number]
MFCD00865948 | [MOL File]
126222-34-2.mol | [Molecular Weight]
630.846 |
| Hazard Information | Back Directory | [Uses]
Remikiren, is a renin inhibitor under development for the treatment of hypertension (high blood pressure). | [Definition]
ChEBI: Remikiren is an L-histidine derivative that is L-histidine in which one of the amino hydrogens is replaced by a (2S)-2-[(2-methylpropane-2-sulfonyl)methyl]-3-phenylpropanoyl group and the carboxy group is replaced by a [(2S,3R,4S)-1-cyclohexyl-4-cyclopropyl-3,4-dihydroxybutan-2-yl]amino group. It is a renin inhibitor which was under development for the treatment of hypertension (now discontinued). It has a role as an antihypertensive agent, a vasodilator agent, a peptidomimetic and an EC 3.4.23.15 (renin) inhibitor. It is a sulfone, a diol, a secondary carboxamide, a member of cyclopropanes and a L-histidine derivative. | [in vivo]
Remikiren (0.1, 0.3, 1, 3, 10 mg/kg; p.o.; single) reduces mean arterial blood pressure in a dose-dependent manner in sodium-depleted marmosets and squirrel monkeys[1].
Remikiren (3 mg/kg; p.o.; single) shows the duration of blood pressure decrease more than 24 h in sodium-depleted marmosets[1]. | Animal Model: | Marmosets and squirrel monkeys (sodium-depleted)[1]. | | Dosage: | 0.1, 0.3, 1, 3, 10 mg/kg | | Administration: | Oral administration; single. | | Result: | Decreased mean arterial pressure (MAP) by 20-25 mm Hg when at 0.1 mg/kg.
Reached the maximal decrease (30 mm Hg) of MAP with 1 mg/kg in marmosets.
Decreasesd 35 mm Hg blood pressure with 3-10 mg/kg in squirrel monkeys.
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| Animal Model: | Marmosets (sodium-depleted)[1]. | | Dosage: | 3 mg/kg | | Administration: | Oral administration; single. | | Result: | Showed MAP fell by 30 mm Hg, which lasting more than 24 h. |
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| Company Name: |
LGM Pharma
|
| Tel: |
1-(800)-881-8210 |
| Website: |
www.lgmpharma.com |
| Company Name: |
Energy Chemical
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| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
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