AZ1136
Based on 1 Customer Validation
AZ1136 is a γ-secretase modulator that regulates amyloid-β (Aβ) production without reducing total Aβ generation. AZ1136 also modulates γ-secretase-mediated Notch S4 cleavage, but does not inhibit NICD formation. AZ1136 can be used in studies related to γ-secretase, APP processing and Alzheimer's disease.
For research use only. We do not sell to patients.
- Purity : 99.91%
- CAS No.: 1380508-60-0
- Formula: C24H21N5O3
- Molecular Weight:427.46
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
AZ1136 modulates γ-secretase-mediated Aβ production in HEK/APPswe cells, potently reduces the levels of amyloidogenic Aβ42 (IC50 = 990 nM) and Aβ40 (IC50 = 1400 nM), while increasing the shorter, less amyloidogenic Aβ37 and Aβ39, without altering total Aβ levels[2].
AZ1136 (25 μM; 16 h) reduces Aβ40 and Aβ42 by 2.3-fold and 8.3-fold, respectively, increases Aβ37 and Aβ39 by 3.5-fold and 2.1-fold, respectively, in HEK/APPswe cells, while Aβ38 remains unaffected[2].
AZ1136 (5 h) modulates γ-secretase-mediated APP processing in HEK/APPswe cells, reduces the levels of Aβ42 (IC50 990 nM) and Aβ40 (IC50 1400 nM) (with higher potency against Aβ42), and increases the shorter Aβ37 and Aβ39 peptides, without altering total Aβ levels or inducing cytotoxicity[3].
AZ1136 (0-5 μM; 5 h) competes with AZ4800 for binding to a common molecular target in HEK/APPswe cells, indicating that both belong to the same class of second-generation γ-secretase modulators[3].
AZ1136 (2 h) retains Aβ-modulating activity in both HEK/APPswe-derived total membranes (TM) and carbonate-extracted membranes (CEM), significantly inhibiting Aβ42 and increasing Aβ37; a slight increase in Aβ38 is also observed in this cell-free membrane assay[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1380508-60-0
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Appearance Solid
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Molecular Weight 427.46
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Formula C24H21N5O3
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Color White to off-white
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SMILES
O=C1C2=CN=C(OC3=CC=C(C4=CN=CO4)C=C3)N=C2N(C)CC(C5=CC=CC=C5)N1C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (116.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Purity & Documentation
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Data Sheet (284 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[2]. Wanngren J, et al. Second generation γ-secretase modulators exhibit different modulation of Notch β and Aβ production. The Journal of biological chemistry. 2012 Sep 21;287(39):32640-50. [Content Brief]
[3]. Borgegard T, et al. First and second generation γ-secretase modulators (GSMs) modulate amyloid-β (Aβ) peptide production through different mechanisms. The Journal of biological chemistry. 2012 Apr 06;287(15):11810-9. [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 |
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| DMSO | 1 mM | 2.3394 mL | 11.6970 mL | 23.3940 mL | 58.4850 mL |
| 5 mM | 0.4679 mL | 2.3394 mL | 4.6788 mL | 11.6970 mL | |
| 10 mM | 0.2339 mL | 1.1697 mL | 2.3394 mL | 5.8485 mL | |
| 15 mM | 0.1560 mL | 0.7798 mL | 1.5596 mL | 3.8990 mL | |
| 20 mM | 0.1170 mL | 0.5849 mL | 1.1697 mL | 2.9243 mL | |
| 25 mM | 0.0936 mL | 0.4679 mL | 0.9358 mL | 2.3394 mL | |
| 30 mM | 0.0780 mL | 0.3899 mL | 0.7798 mL | 1.9495 mL | |
| 40 mM | 0.0585 mL | 0.2924 mL | 0.5849 mL | 1.4621 mL | |
| 50 mM | 0.0468 mL | 0.2339 mL | 0.4679 mL | 1.1697 mL | |
| 60 mM | 0.0390 mL | 0.1950 mL | 0.3899 mL | 0.9748 mL | |
| 80 mM | 0.0292 mL | 0.1462 mL | 0.2924 mL | 0.7311 mL | |
| 100 mM | 0.0234 mL | 0.1170 mL | 0.2339 mL | 0.5849 mL |
AZ1136 Related Classifications
HY-128391 Related Classifications
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