GLPBio

ACT 178882

Catalog No.: GC31621Purity:>98.00%
COASDSData Sheet
ACT 178882 es un nuevo inhibidor de Renina con un IC50 de 1,4 nM.

Los productos son exclusivamente para uso en investigación. No aptos para uso humano. No vendemos a pacientes.

ACT 178882
Cas No.: 1007392-69-9
1mgIn Stock
$3,990.00
1
5mgIn Stock
$9,855.00
1
10mgIn Stock
$16,887.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

Citas (Citations)

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    Nature
    641, 529–536 (2025)
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    Nature
    628, 630–638 (2024)
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    Nature
    632, 686–694 (2024)
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    Nature
    618, 1017–1023 (2023)
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    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
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    Science
    388(6745) (2025)
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    387(6739) (2025)
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    Science
    387(6734) (2025)
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    Cell Research
    35, 97–116 (2025)
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    Cell Research
    34, 683–706 (2024)
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    33, 273–287 (2023)
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    33, 546–561 (2023)
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    33, 904–922 (2023)
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    Cell Research
    31, 1291–1307 (2021)

Descripción (Description)

ACT 178882 is a new Renin inhibitor with an IC50 of 1.4 nM.

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].

[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.

Protocolo (Protocol)

Cell experiment:

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.

Documentos del producto (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Propiedades químicas (Chemical Properties)

N.º CAS
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
Fórmula molecular
C33H38Cl3N3O4
Peso molecular
647.03
Solubilidad
Soluble in DMSO
Almacenamiento
Store at -20°C
Consejos generales
Seleccione un disolvente adecuado según los datos de solubilidad del producto. Una vez preparada, divida la solución madre en alícuotas para evitar ciclos repetidos de congelación y descongelación.
Utilice las soluciones madre en un plazo de 6 meses si se conservan a -80°C, o de 1 mes si se conservan a -20°C.
Para mejorar la solubilidad, caliente el tubo a 37°C y soníquelo durante un periodo adecuado.
Condiciones de envío
Las muestras de evaluación se envían con acumuladores de frío. Los demás tamaños se envían a temperatura ambiente o, previa solicitud, con acumuladores de frío.

Calculadoras (Calculators)Molaridad / Dilución / Peso molecular / Conversión de unidades / Formulación in vivo / Solubilidad

g/mol

Reviews

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