1. Metabolic Enzyme/Protease
  2. Renin
  3. Remikiren

Remikiren (Ro 42-5892) is an orally active and highly specific renin inhibitor. Remikiren specifically inhibits human reninand human plasma renin with IC50 values of 0.7 and 0.8 nM, respectively. Remikiren also reduces mean arterial blood pressure in sodium-depleted marmosets and squirrel monkeys. Remikiren can be used in study of hypertension.

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Remikiren

Remikiren Chemical Structure

CAS No. : 126222-34-2

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Description

Remikiren (Ro 42-5892) is an orally active and highly specific renin inhibitor. Remikiren specifically inhibits human reninand human plasma renin with IC50 values of 0.7 and 0.8 nM, respectively. Remikiren also reduces mean arterial blood pressure in sodium-depleted marmosets and squirrel monkeys. Remikiren can be used in study of hypertension[1].

IC50 & Target

IC50:0.7 nM (human pure renin), 0.8 nM (plasma renin of human)[1].

In Vitro

Remikiren (0-10 nM; 1-3 h) displays a considerable specificity to inhibit renin[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Human pure renin, plasma renin of human, marmoset, squirrel monkey
Concentration: 0-10 nM
Incubation Time: 1-3 h
Result: Inhibited human pure renin and plasma renin of human, marmoset, squirrel monkey with IC50 values of 0.7, 0.8, 1.0 and 1.7 nM, respectively.
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Masse moléculaire

630.84

Formule

C33H50N4O6S

CAS No.
SMILES

CC(C)(C)S(C[C@@H](CC1=CC=CC=C1)C(N[C@@H](CC2=CN=CN2)C(N[C@H]([C@@H](O)[C@H](C3CC3)O)CC4CCCCC4)=O)=O)(=O)=O

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation
Références
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Nom du produit:
Remikiren
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HY-A0184
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