ACT 178882
ACT 178882 is a new Renin inhibitor with an IC50 of 1.4 nM.
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- CAS No.: 1007392-69-9
- Formule: C33H38Cl3N3O4
- Masse moléculaire:647.03
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
IC50: 1.4 nM (Renin)[1]
The median time to Cmax (tmax) for ACT 178882 is prolonged from 3.5 to 5.0 h by diltiazem whereas its apparent terminal half-life (t?) is unaffected by diltiazem, 22.9 and 24.2 h for treatments A and B, respectively. Using treatment A as reference, the geometric mean ratio (90% CI) is 1.62 (1.36 to 1.94) for Cmax and 2.02 (1.75 to 2.34) for AUC∞, indicating a significant interaction between ACT 178882 and diltiazem[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1007392-69-9
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Masse moléculaire 647.03
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Formule C33H38Cl3N3O4
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SMILES
O=C([C@H]1CNCC[C@@H]1C2=CC=C(OCCOC3=C(Cl)C=C(C)C=C3Cl)N=C2)N(CC4=CC(CCOC)=CC=C4Cl)C5CC5
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
Venous blood samples for the determination of ACT 178882 are drawn at the following time points: pre-dose and 1, 2, 3, 4, 5, 6, 8, 12, 16, 24, 36, 48, 72, 96 and 120 h after dosing with ACT 178882 in treatment A and pre-dose and 1, 2, 3, 4, 5, 6, 8, 12, 16, 24, 36, 48, 72, 96, 120, 144, 168, 192, 216 and 240 h after dosing with ACT178882 in treatment B. For diltiazem as soon as possible after collection, and for ACT-178882 within maximally 30 minutes after collection, the tubes are centrifuged and the plasma separated. All samples are stored in an upright position at -20 °C (ACT 178882) or -80 °C (diltiazem) or below pending analysis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
Références
[1]. Corminboeuf O, et al. Piperidine-based renin inhibitors: upper chain optimization. Bioorg Med Chem Lett. 2010 Nov 1;20(21):6291-6. [Content Brief]
[2]. Dingemanse J, et al. Drug-drug interaction study of ACT-178882, a new renin inhibitor, and diltiazem in healthy subjects. Clin Drug Investig. 2013 Mar;33(3):207-13. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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