ACT 178882
ACT 178882 is a new Renin inhibitor with an IC50 of 1.4 nM.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1007392-69-9
- 分子式: C33H38Cl3N3O4
- 分子量:647.03
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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.
化学情報
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CAS 番号 1007392-69-9
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分子量 647.03
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
ACT 178882 関連分類
HY-U00262 関連分類
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