N-desethyl Amodiaquine (hydrochloride) |
| رقم الكتالوجGC44344 |
N-desethyl Amodiaquine (هيدروكلوريد) هو المستقلب الرئيسي النشط بيولوجيًا للأمودياكين.
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-desethyl Amodiaquine (hydrochloride) (DEAQ) is the major metabolite of the antimalarial compound aminodiaquine, produced by the action of cytochrome P450 isoform 2C8 [1]. N-desethyl Amodiaquine (hydrochloride) is an antiparasitic agent that is highly active against Plasmodium falciparum and can synergize with amodiaquine[2]. N-desethyl Amodiaquine (hydrochloride) has inhibitory effects against strains V1/S and 3D7 with IC50 values of 97 nM and 25 nM, respectively [3]. This product is provided as N-desethyl Amodiaquine hydrochloride.
In vitro, treatment with N-desethyl Amodiaquine (hydrochloride) significantly blocked viral replication in both Huh 7 and Vero E6 cell lines infected with Ebola virus, with IC50 values in the low μM range [4]. Treatment of RAW264.7 cells with N-desethyl Amodiaquine (hydrochloride) (4, 8, 16, 33, 66 μM) for 1 h inhibited proteinase B activity in a dose-dependent manner[5].
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.
Cell experiment [1]: | |
Cell lines | RAW264.7 cells |
Preparation method | RAW264.7 cells were treated with N-desethyl Amodiaquine (hydrochloride)(4, 8, 16, 33, or 66μM) for 1 hour prior to lysis and determination of cathepsin B activity. |
Reaction Conditions | 4, 8, 16, 33, or 66μM; 1 h |
Applications | Cells pre-treated with N-desethyl Amodiaquine (hydrochloride) for 1 hour lost cathepsin B enzymatic activity in a dose dependent manner. |
References: [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 |
| الذوبان | 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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4956 mL | 12.4782 mL | 24.9563 mL |
| 5 mM | 499.1 μL | 2.4956 mL | 4.9913 mL |
| 10 mM | 249.6 μL | 1.2478 mL | 2.4956 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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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