N-desethyl Amodiaquine (hydrochloride) |
| カタログ番号GC44344 |
N-デセチルアモジアキン（塩酸塩）（N-desethyl Amodiaquine (hydrochloride)）（DEAQ）は、抗マラリア薬アミノジアキンの主要な代謝物であり、シトクロムP450アイソフォーム2C8の作用によって生成される。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 79049-30-2
Sample solution is provided at 25 µL, 10mM.
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N-デセチルアモジアキン（塩酸塩）（N-desethyl Amodiaquine (hydrochloride)）（DEAQ）は、抗マラリア薬アミノジアキンの主要な代謝物であり、シトクロムP450アイソフォーム2C8の作用によって生成される。N-デセチルアモジアキン（塩酸塩）は、Plasmodium falciparumに対して高い活性を持つ抗寄生虫剤であり、アモジアキンと相乗効果を示すことがある。N-デセチルアモジアキン（塩酸塩）は、V1/Sおよび3D7株に対してそれぞれIC50値97 nMおよび25 nMの阻害効果を持つ。本製品はN-デセチルアモジアキン塩酸塩として提供される。
In vitroでは、N-デセチルアモジアキン（塩酸塩）の処理により、エボラウイルスに感染したHuh 7およびVero E6細胞株のウイルス複製が有意に阻害され、IC50値は低μM範囲であった。RAW264.7細胞をN-デセチルアモジアキン（塩酸塩）（4, 8, 16, 33, 66 μM）で1時間処理すると、プロテアーゼB活性が用量依存的に阻害された。
References:
[1] Li X Q, Björkman A, Andersson T B, et al. Amodiaquine clearance and its metabolism ton-desethylamodiaquine is mediated by CYP2C8: a new high affinity and turnover enzyme-specific probe substrate[J]. Journal of Pharmacology and Experimental Therapeutics, 2002, 300(2): 399-407.
[2] Mariga S T, Gil J P, Sisowath C, et al. Synergism between amodiaquine and its major metabolite, desethylamodiaquine, against Plasmodium falciparum in vitro[J]. Antimicrobial agents and chemotherapy, 2004, 48(11): 4089-4096.
[3] Sasi P, Abdulrahaman A, Mwai L, et al. In vivo and in vitro efficacy of amodiaquine against Plasmodium falciparum in an area of continued use of 4-aminoquinolines in East Africa[J]. The Journal of infectious diseases, 2009, 199(11): 1575-1582.
[4] DeWald L E, Johnson J C, Gerhardt D M, et al. In vivo activity of amodiaquine against Ebola virus infection[J]. Scientific Reports, 2019, 9(1): 20199.
[5] Zilbermintz L, Leonardi W, Jeong S Y, et al. Identification of agents effective against multiple toxins and viruses by host-oriented cell targeting[J]. Sci Rep. 2015.
| 細胞実験[1]: | |
細胞株 | RAW264.7 細胞 |
準備方法 | RAW264.7 細胞をN-デセチルアモジアキン（塩酸塩）（4, 8, 16, 33, 66 μM）で1時間処理し、細胞溶解後にカテプシンB活性を測定した。 |
反応条件 | 4, 8, 16, 33, 66 μM; 1時間 |
アプリケーション | N-デセチルアモジアキン（塩酸塩）を1時間前処理した細胞は、用量依存的にカテプシンBの酵素活性を失った。 |
参考文献: [1]Zilbermintz L, Leonardi W, Jeong S Y, et al. Identification of agents effective against multiple toxins and viruses by host-oriented cell targeting[J]. Sci Rep. 2015. | |
| Cas No. | 79049-30-2 | SDF | |
| Canonical SMILES | OC(C=C1)=C(CNCC)C=C1NC2=CC=NC3=C2C=CC(Cl)=C3.Cl.Cl | ||
| Formula | C18H18ClN3O•2HCl | M.Wt | 400.7 |
| 溶解度 | DMSO: soluble,Methanol: Soluble,Water: Soluble | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4956 mL | 12.4782 mL | 24.9563 mL |
| 5 mM | 0.4991 mL | 2.4956 mL | 4.9913 mL |
| 10 mM | 0.2496 mL | 1.2478 mL | 2.4956 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)
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