NCO-700
NCO-700 is a dual cathepsin B and calcium-activated neutral protease (CANP) inhibitor with IC50 values of 0.8 and 46 μM, respectively. NCO-700 reduces the degradation of myocardial fibrin by inhibiting protease activity. NCO-700 also has inhibitory effects on hormone-independent tumor cells, such as prostate cancer cells, and induces apoptosis. NCO-700 can be used to study myocardial ischemia and refractory hormone-independent tumors.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 84518-80-9
- 分子式: C26H39N3O8
- 分子量:521.60
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Cathepsin アイソフォーム固有の製品をすべて表示
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生物活性
NCO-700 (7 days) inhibits HS-578T, PC-3, DU-145, MCF-7, LNCaP and T47D cells proliferation with IC50s of 7.5, 10, 11.5, 72 and >100 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
NCO-700 (10-100 mg/kg, i.p., once daily for 5 days) demonstrates significant anti-tumor activity in xenograft models of prostate cancer and breast cancer in mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:
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Dosage:20 and 40 mg/kg (total dose)
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Administration:Intraperitoneal injection (i.p.), 4 administrations of medication
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Result:Reduced the infarcted area by 11.5% and 22.3% at 20 and 40 mg/kg in rabbit model.
Significantly inhibited the degradation of myofibrillar proteins induced by ischemia in dog model.
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Animal Model:Xenograft models of prostate cancer and breast cancer established in Balb/C mice[2]
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Dosage:10, 20 and 40 mg/kg (prostate cancer) and 10, 50 and 100 mg/kg (breast cancer)
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Administration:Intraperitoneal injection (i.p.), once daily for 5 days
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Result:Significantly slowed down the growth rate of the tumor.
Induced cell apoptosis in cancer cells removed from animals.
化学情報
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CAS 番号 84518-80-9
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分子量 521.60
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分子式 C26H39N3O8
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SMILES
O=C(N1CCN(CC2=C(C(OC)=C(OC)C=C2)OC)CC1)[C@H](CC(C)C)NC([C@H]3[C@H](C(OCC)=O)O3)=O
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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.
純度とドキュメンテーション
参考文献
[1]. Toyo-oka T, et al. Reduction of experimentally produced acute myocardial infarction size by a new synthetic inhibitor, NCO-700, against calcium-activated neutral protease. Jpn Heart J. 1982 Sep;23(5):829-34. [Content Brief]
[2]. Eilon GF, et al. Tumor apoptosis induced by epoxide-containing piperazines, a new class of anti-cancer agents. Cancer Chemother Pharmacol. 2000;45(3):183-91. [Content Brief]
[3]. Sashida H, Abiko Y. Inhibition with NCO-700, a protease inhibitor, of degradation of cardiac myofibrillar proteins during ischemia in dogs. Biochem Pharmacol. 1985 Nov 1;34(21):3875-80. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)