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Chemical Structure| 870843-42-8 Chemical Structure| 870843-42-8

Structure of E 2012
CAS No.: 870843-42-8

Chemical Structure| 870843-42-8

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E 2012 is a potent γ-secretase modulator.

Synonyms: E 2012

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Product Details of E 2012

CAS No. :870843-42-8
Formula : C25H26FN3O2
M.W : 419.49
SMILES Code : O=C1N([C@H](C2=CC=C(F)C=C2)C)CCC/C1=C\C3=CC=C(N4C=C(C)N=C4)C(OC)=C3
Synonyms :
E 2012
MDL No. :MFCD11042274
InChI Key :PUOAETJYKQITMO-LANLRWRYSA-N
Pubchem ID :11560787

Safety of E 2012

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H317-H319
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
mouse pancreatic acinar cells 266-6 2 μM 48 hours To investigate the role of Traf6 in caerulein-induced pancreatitis, it was found that overexpression of Traf6 significantly reduced PARP and caspase-3 cleavage, indicating that Traf6 has a protective effect against apoptosis PMC4720878
mouse pancreatic acinar cells 266-6 0.25 –4 μM 48 hours To investigate the effect of LPS on Traf6 expression, it was found that LPS increased Traf6 expression at low concentrations (≤0.5μM), but significantly suppressed Traf6 expression at high concentrations (>1 μM) PMC4720878
H4-APP cells 1 μM 1 hour E2012-BPyne specifically labels PS1-NTF, and the labeling is competed in the presence of E2012 but not with GSM-1. PMC3617273
ANP.24 cells 1 μM 1 hour E2012-BPyne preferentially labels active PS1-NTF over inactive full-length PS1. PMC3617273
Primary neuronal cultures 2 μM 1 hour E2012-BPyne labels PS1-NTF in primary neuronal cultures, and the labeling is significantly enhanced in the presence of L458. PMC3617273

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Beagle dogs Oral 10 mg/kg 1 hour before administration, lasted for 24 hours To investigate the effect of E2012 on APLP1 processing, results showed a dose-dependent relative increase of CSF peptides APLP1 β17, 1 β18, and 1 β28 accompanied by a decrease in 1 β25 and 1 β27 in response to E2012 treatment PMC4687145
mice acute edematous pancreatitis (AEP) and acute necrotizing pancreatitis (ANP) models intraperitoneal injection 12 mg/kg 2 days per week for 30 days To investigate the role of Traf6 in different pancreatitis models, it was found that Traf6 expression increased in mild pancreatitis but decreased in severe pancreatitis, indicating that Traf6 plays a protective role in the progression of pancreatitis PMC4720878

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.38mL

0.48mL

0.24mL

11.92mL

2.38mL

1.19mL

23.84mL

4.77mL

2.38mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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