gamma-secretase modulator 5
gamma-secretase modulator 5 (compound 22d) is a brain-penetrant gamma-secretase modulator (GSMs) that inhibits the production of the aggregated amyloid β-peptide Aβ42 with an IC50 value of 60 nM. gamma-secretase modulator 5 can be used in the study of Alzheimer's disease.
For research use only. We do not sell to patients.
- CAS No.: 1353570-53-2
- Formula: C22H25N7OS
- Molecular Weight:435.55
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Aβ38 305 nM (EC50) |
Aβ40 104 nM (IC50) |
Aβ42 60 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SH-SY5Y | EC50 |
30 nM
Compound: 45
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Modulation of gamma-secretase in human SH-SY5Y cells expressing human APP751 assessed as reduction in amyloid beta 42 production after 24 hrs by sandwich ELISA
Modulation of gamma-secretase in human SH-SY5Y cells expressing human APP751 assessed as reduction in amyloid beta 42 production after 24 hrs by sandwich ELISA
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[PMID: 27007185] |
gamma-secretase modulator 5 (compound 22d) (1-10 μM, 24 h) does not affect the function of the APP751 enzyme and not inhibit Notching processing in H4 human neuroglioma cells over-expressing human APP751[1].
gamma-secretase modulator 5 (compound 22d) acts on Aβ38 with the EC50 value of 305 nM and acts on Aβ40 with the IC50 value of 104 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Parameters | IV | PO |
| Dose (mg/kg) | 1 | 5 |
| Cmax (ng/mL) | 824 | 705 |
| Tmax (h) | 0.083 | 0.25 |
| t1/2 (h) | 0.5 | - |
| AUClast (ng•h/mL) | 443 | 1089 |
| AUCinf (ng•h/mL) | 463 | 1243 |
| Cl (mL/h/kg) | 2159 | - |
| Vss (mL/kg) | 1413 | - |
| F (%) | 100 | 53.7 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1353570-53-2
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Molecular Weight 435.55
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Formula C22H25N7OS
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SMILES
CC1=CN(C2=CC=C(C3=CSC(NC4=C5C(CCCC5)=NN4CC)=N3)N=C2OC)C=N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
gamma-secretase modulator 5 Related Classifications
HY-150050 Related Classifications
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