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A cell-permeable purine compound that acts as a highly potent and selective inhibitor against γ-secretase-mediated production of Aβ42 over Aβ40 (IC50 = 21 and 350 nM, respectively) and Notch1 (Notch IC50/ Aβ42 IC50 >2400) in cultures in vitro. Reported to be blood-brain barrier-permeant and orally bioavailable in APP-YAC transgenic mice and effectively reduce Aβ42 (by 73%), but not Aβ40, level in brain (100 mg/kg, p.o.) in vivo.
Catalogue Number
565792
Brand Family
Calbiochem®
References
References
Rivkin, A., et al. 2010. Bioorg. Med. Chem. Lett.20, 2279.
Rivkin, A., et al. 2010. Bioorg. Med. Chem. Lett.20, 2279.
数据表
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
24-June-2011 JSW
Description
A cell-permeable purine compound that acts as a highly potent and selective inhibitor against γ-secretase-mediated production of Aβ42 over Aβ40 (IC50 = 21 and 350 nM, respectively) and Notch1 (Notch IC50/ Aβ42 IC50 >2400) in cultures in vitro. Reported to be blood-brain barrier-permeant and orally bioavailable in APP-YAC transgenic mice and effectively reduce Aβ42 (by 73%), but not Aβ40, level in brain (100 mg/kg, p.o.) in vivo.
Form
Beige solid
Intert gas (Yes/No)
Packaged under inert gas
Chemical formula
C₃₀H₃₉N₇O
Structure formula
Purity
≥95% by HPLC
Solubility
DMSO (25 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2 months at -20°C.
Toxicity
Standard Handling
References
Rivkin, A., et al. 2010. Bioorg. Med. Chem. Lett.20, 2279.
