1007392-69-9

1007392-69-9 structure

1007392-69-9 structure

Name: ACT 178882
Chemical Name: ACT 178882
CAS Number: 1007392-69-9
Molecular Formula: C₃₃H₃₈Cl₃N₃O₄
Molecular Weight: 647.031
Catalog: Signaling Pathways Metabolic Enzyme/Protease Renin
Create Date: 2018-01-10 08:31:19
Modify Date: 2024-02-26 19:53:25
ACT 178882 is a new Renin inhibitor with an IC50 of 1.4 nM.

Name	ACT 178882
Synonyms	(3R,4S)-N-[2-Chloro-5-(2-methoxyethyl)benzyl]-N-cyclopropyl-4-{6-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-3-pyridinyl}-3-piperidinecarboxamide 3-Piperidinecarboxamide, N-[[2-chloro-5-(2-methoxyethyl)phenyl]methyl]-N-cyclopropyl-4-[6-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]-3-pyridinyl]-, (3R,4S)-

Description	ACT 178882 is a new Renin inhibitor with an IC50 of 1.4 nM.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Renin Research Areas >> Metabolic Disease
Target	IC50: 1.4 nM (Renin)[1]
In Vitro	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 (t½) 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].
Cell Assay	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].
References	[1]. Corminboeuf O, et al. Piperidine-based renin inhibitors: upper chain optimization. Bioorg Med Chem Lett. 2010 Nov 1;20(21):6291-6. [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.

Density	1.3±0.1 g/cm3
Boiling Point	764.3±60.0 °C at 760 mmHg
Molecular Formula	C₃₃H₃₈Cl₃N₃O₄
Molecular Weight	647.031
Flash Point	416.0±32.9 °C
Exact Mass	645.192810
LogP	6.12
Vapour Pressure	0.0±2.6 mmHg at 25°C
Index of Refraction	1.623