β-Secretase Inhibitor IV |
Catalog No.GC18464
One-Click Copy Product Info
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β-Secretase Inhibitor IV se lie au site actif de BACE-1 et bloque efficacement son activité protéolytique (IC₅₀=15nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 797035-11-1
Sample solution is provided at 25 µL, 10mM.
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β-Secretase Inhibitor IV se lie au site actif de BACE-1 et bloque efficacement son activité protéolytique (IC₅₀=15nM). β-Secretase Inhibitor IV réduit la production du peptide amyloïde-β par l'inhibition du site de clivage de la β-sécrétase de la protéine précuseur de l'amyloïde. β-Secretase Inhibitor IV peut être utilisé dans l'étude sur les maladies neurodégénératives comme la maladie d' Alzheimer[3-4].
In vitro, β-Secretase Inhibitor IV (0.36μM) a été incubé avec des cellules murines Neuro2a (N2a) durant 24 heures, ce qui a inhibé la sécrétion du peptide amyloïde-β Aβ40[5]. β-Secretase Inhibitor IV (29nM) a été incubé avec des cellules HEK293FT durant 6 heures. β-Secretase Inhibitor IV a fortement inhibé l'activité intracellulaire de BACE-1[6].
In vivo, une injection intrapéritonéale unique de β-Secretase Inhibitor IV (8mg/kg) a été administrée à des souris transgéniques Tg2576 qui expriment la protéine précuseur de l'amyloïde (APP). Après 4 heures, β-Secretase Inhibitor IV a fortement réduit les taux plasmatiques d' Aβ40[7].
References:
[1] Z Pietrak BL, Crouthamel MC, Tugusheva K, et al. Biochemical and cell-based assays for characterization of BACE-1 inhibitors. Anal Biochem. 2005 Jul 1;342(1):144-51.
[2] Cheng XR, Zhou JW, Zhou Y, et al. The green tea polyphenol (2)-epigallocatechin-3-gallate (EGCG) is not a β-secretase inhibitor. Bioorg Med Chem Lett. 2012 Feb 1;22(3):1408-14.
[3] Zhu YP, Xiao K, Yu HP, et al. Discovery of potent beta-secretase (bace-1) inhibitors by the synthesis of isophthalamide-containing hybrids. Acta Pharmacol Sin. 2009 Feb;30(2):259-69.
[4] Nordeman P, Estrada S, Odell LR, et al. (11)C-Labeling of a potent hydroxyethylamine BACE-1 inhibitor and evaluation in vitro and in vivo. Nucl Med Biol. 2014 Jul;41(6):536-43.
[5] Garino C, Tomita T, Pietrancosta N, et al. Naphthyl and coumarinyl biarylpiperazine derivatives as highly potent human beta-secretase inhibitors. Design, synthesis, and enzymatic BACE-1 and cell assays. J Med Chem. 2006 Jul 13;49(14):4275-85.
[6] Choi SJ, Cho JH, Im I, et al. Design and synthesis of 1,4-dihydropyridine derivatives as BACE-1 inhibitors. Eur J Med Chem. 2010 Jun;45(6):2578-90.
[7] Ghosh AK, Kumaragurubaran N, Hong L, et al. Design, synthesis, and X-ray structure of potent memapsin 2 (beta-secretase) inhibitors with isophthalamide derivatives as the P2-P3-ligands. J Med Chem. 2007 May 17;50(10):2399-407.
| Expériences cellulaires [1]: | |
Lignées cellulaires | les cellules Neuro2a (N2a) murines (lignée cellulaire de neuroblastome murin) |
Méthode de préparation | les cellules ont été ensemencées dans des plaques de 24 puits ont été cultivées jusqu'à la confluence. β-Secretase Inhibitor IV a été dilué à partir d'une solution mère dans DMSO dans le milieu de culture pour atteindre une concentration finale de 0.1% de DMSO. |
Conditions de réaction | 0.36μM; 24h. |
Domaines d'application | β-Secretase Inhibitor IV a inhibé la sécrétion du peptide amyloïde-β Aβ40 par les cellules. |
| Expériences animales [2]: | |
Modèles animaux | des souris transgéniques Tg2576 (un modèle de la maladie d' Alzheimer) |
Méthode de préparation | Les souris ont reçu une administration intrapéritonéale (i.p.) unique de β-Secretase Inhibitor IV (8mg/kg). |
Forme de dosage | 8mg/kg; i.p.; une injection unique |
Domaines d'application | L'administration de β-Secretase Inhibitor IV entraîne une réduction 30% des taux plasmatiques d' Aβ40 à 4 heures après l'injection. L'inhibition observée de la production d' Aβ40 était notable. |
References: | |
| Cas No. | 797035-11-1 | SDF | |
| Chemical Name | N1-[(1S,2R)-3-(cyclopropylamino)-2-hydroxy-1-(phenylmethyl)propyl]-5-[methyl(methylsulfonyl)amino]-N3-[(1R)-1-phenylethyl]-1,3-benzenedicarboxamide | ||
| Canonical SMILES | CN(S(C)(=O)=O)C1=CC(C(N[C@H](C)C2=CC=CC=C2)=O)=CC(C(N[C@@H](CC3=CC=CC=C3)[C@H](O)CNC4CC4)=O)=C1 | ||
| Formula | C31H38N4O5S | M.Wt | 578.7 |
| Solubility | 10mg/mL in ethanol, 20mg/mL in DMSO or in DMF | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.728 mL | 8.6401 mL | 17.2801 mL |
| 5 mM | 345.6 μL | 1.728 mL | 3.456 mL |
| 10 mM | 172.8 μL | 864 μL | 1.728 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
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 saline, 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% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 11 reference(s) in Google Scholar.)