AZD3839 |
Catalog No.GC15715
One-Click Copy Product Info
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BACE1 inhibitor,potent and selective
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1227163-56-5
Sample solution is provided at 25 µL, 10mM.
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AZD3839 is a novel inhibitor of BACE1 with IC50 value of 4.8μM [1].
AZD3839 has been reported to inhibit human BACE1 activity in a biochemical FRET assay. In addition, AZD3839 has also been reported to inhibit the release of sAPPβs from human SH-SY5Y cells, mouse N2A cells and mouse and guinea pig primary cortical neurons. Moreover, AZD3839 has been revealed to effectively decrease the cerebrospinal fluid (CSF), plasma, and brain Aβ levels in guinea pig, mouse and non-human primate. AZD3839 has also been revealed to decrease the levels of Aβ40 secreted from C57BL/6 mouse primary cortical neurons, N2A cells (mouse neuroblastoma), and Dunkin-Hartley guinea pig primary cortical neurons, with IC50 values of 50.9, 32.2, and 24.8 nmol/liter, respectively [2].
References:
[1] Sparve E1, Quartino AL1, Luttgen M1, Tunblad K1, Teiling-Gardlund A1, Falting J1, Alexander R1, Kagstrom J1, Sjodin L1, Bulgak A1, Al-Saffar A1, Bridgland-Taylor M2, Pollard C3, Swedberg MD4, Vik T5, Paulsson B1. Prediction and modeling of effects on the QTc interval for clinical safety margin assessment, based on Single Ascending Dose study data with AZD3839. J Pharmacol Exp Ther. 2014 Jun 10.
[2] Jeppsson F1, Eketjäll S, Janson J, Karlström S, Gustavsson S, Olsson LL, Radesäter AC, Ploeger B, Cebers G, Kolmodin K, Swahn BM, von Berg S, Bueters T, Fälting J. Discovery of AZD3839, a potent and selective BACE1 inhibitor clinical candidate for the treatment of Alzheimer disease. J Biol Chem. 2012 Nov 30;287(49):41245-57.
| Cas No. | 1227163-56-5 | SDF | |
| Chemical Name | (3S)-3-[2-(difluoromethyl)pyridin-4-yl]-7-fluoro-3-(3-pyrimidin-5-ylphenyl)-1,2-dihydroisoindol-1-amine | ||
| Canonical SMILES | C1=CC(=CC(=C1)C2(C3=C(C(N2)N)C(=CC=C3)F)C4=CC(=NC=C4)C(F)F)C5=CN=CN=C5 | ||
| Formula | C24H15F4N5 | M.Wt | 449.4 |
| Solubility | DMF: 2 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,Ethanol:PBS (pH 7.2) (1:1): 0.5 mg/ml | 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 | 2.2252 mL | 11.1259 mL | 22.2519 mL |
| 5 mM | 445 μL | 2.2252 mL | 4.4504 mL |
| 10 mM | 222.5 μL | 1.1126 mL | 2.2252 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 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 4 reference(s) in Google Scholar.)