ACT 178882

Cat. No.: HY-U00262: FAQs
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ACT 178882 is a new Renin inhibitor with an IC₅₀ of 1.4 nM.

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ACT 178882 Chemical Structure

CAS No. : 1007392-69-9

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Description	ACT 178882 is a new Renin inhibitor with an IC₅₀ of 1.4 nM.
IC₅₀ & Target	IC50: 1.4 nM (Renin)^[1]
In Vitro	The median time to C_max (t_max) 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 C_max 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. ACT 178882 Related Antibodies
Molecular Weight	647.03
Formula	C₃₃H₃₈Cl₃N₃O₄
CAS No.	1007392-69-9
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
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation	Data Sheet (275 KB) Handling Instructions (2659 KB)
References	[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]

Cell Assay
^[2]

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].

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

References

[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]

ACT 178882 Related Classifications

Metabolic Disease

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Do most proteins show cross-species activity?
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.

Keywords:

ACT 1788821007392-69-9ACT178882ACT-178882ReninInhibitorinhibitorinhibit

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