Remikiren
Remikiren Basic information
- Product Name:
- Remikiren
- Synonyms:
-
- (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
- Ro-42-5892
- C07465
- Remikiren
- 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)-
- AC1O44IV
- CHEMBL31601
- D09038
- CAS:
- 126222-34-2
- MF:
- C33H50N4O6S
- MW:
- 630.846
- Mol File:
- 126222-34-2.mol
Remikiren Usage And Synthesis
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. |
| 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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