cis-ACCP
Based on 1 Customer Validation
cis-ACCP is an orally active antimetastatic matrix metalloproteinase-2 (MMP-2) selective inhibitor. cis-ACCP can inhibit MMP-2 and MMP-9 with IC50 values of 4 μM and 20 μM, respectively. cis-ACCP can be used for the research of a variety of chronic diseases.
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。
- 純度: 97.0%
- CAS 番号: 777075-44-2
- 分子式: C7H15N2O4P
- 分子量:222.18
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
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MMP-2 4 μM (IC50) |
MMP-9 20 μM (IC50) |
cis-ACCP (oral, i.v.,i.p.; 50, 150 mg/kg) only has distribution in the extracellular fluid[1].
Pharmacokinetic Parameters of cis-ACCP in rats[1].
| PK parameter | iv | PO | ip |
| AUC (min • µg/mL) | 7637 | 79 | 2677 |
| T1/2 (min) | 18.8 | 126 | 108 |
| Cmax(ng/mL) | 306000 | 712 | 144000 |
| CL (mL/min/kg) | 6.9 | - | - |
| Tmax(min) | - | 17.4 | 0.5 |
| Vss(mL/Kg) | 186 | - | - |
| F (%) | - | 0.35 | 11.8 |
| Fu (%) | 83.9 | 2.2 | 48 |
| Ttime over MIC (hr) | >4 | >6 | 24 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL mice[1]
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Dosage:50, 250, 500 mg/kg; 12.5 to 50 mg/kg
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Administration:Oral, intraperitoneal, daily for two weeks; daily, 21 days
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Result:Showed no toxic effects and showed 50-85% inhibition of metastasis formation, depending on the dose.
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Animal Model:Rats[1]
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Dosage:50, 150 mg/kg
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Administration:Oral, intravenous, intraperitoneal
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Result:Showed 84% of the intravenously administered drug are excreted unchanged.
化学情報
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CAS 番号 777075-44-2
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性状 Solid
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分子量 222.18
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分子式 C7H15N2O4P
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Color White to off-white
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SMILES
OP(O)(C(N[C@H]1[C@@H](N)CCCC1)=O)=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
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
H2O : 25 mg/mL (112.52 mM; ultrasonic and warming and heat to 60°C)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
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- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Hoffman, Amnon et al. Carbamoylphosphonate matrix metalloproteinase inhibitors 6: cis-2-aminocyclohexylcarbamoylphosphonic acid, a novel orally active antimetastatic matrix metalloproteinase-2 selective inhibitor--synthesis and pharmacodynamic and pharmacokinetic analysis. Journal of medicinal chemistry vol. 51,5 (2008): 1406-14. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 4.5009 mL | 22.5043 mL | 45.0086 mL | 112.5214 mL |
| 5 mM | 0.9002 mL | 4.5009 mL | 9.0017 mL | 22.5043 mL | |
| 10 mM | 0.4501 mL | 2.2504 mL | 4.5009 mL | 11.2521 mL | |
| 15 mM | 0.3001 mL | 1.5003 mL | 3.0006 mL | 7.5014 mL | |
| 20 mM | 0.2250 mL | 1.1252 mL | 2.2504 mL | 5.6261 mL | |
| 25 mM | 0.1800 mL | 0.9002 mL | 1.8003 mL | 4.5009 mL | |
| 30 mM | 0.1500 mL | 0.7501 mL | 1.5003 mL | 3.7507 mL | |
| 40 mM | 0.1125 mL | 0.5626 mL | 1.1252 mL | 2.8130 mL | |
| 50 mM | 0.0900 mL | 0.4501 mL | 0.9002 mL | 2.2504 mL | |
| 60 mM | 0.0750 mL | 0.3751 mL | 0.7501 mL | 1.8754 mL | |
| 80 mM | 0.0563 mL | 0.2813 mL | 0.5626 mL | 1.4065 mL | |
| 100 mM | 0.0450 mL | 0.2250 mL | 0.4501 mL | 1.1252 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.