Home Proteases Secretase modulator Itanapraced (CHF 5074) For research use only.

Itanapraced (CHF 5074)

Synonyms: CSP-1103

Itanapraced (CHF 5074, CSP-1103) is a gamma-secretase modulator that reduces Aβ42 and Aβ40 secretion. The IC50s of CHF5074 for inhibition of COX-1 and COX-2 is above 100 μmol/L.

Itanapraced (CHF 5074) Chemical Structure

Itanapraced (CHF 5074) Chemical Structure

CAS: 749269-83-8

Purity & Quality Control

Batch: Purity: 99.86%
99.86

Itanapraced (CHF 5074) Related Products

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Biological Activity

Description Itanapraced (CHF 5074, CSP-1103) is a gamma-secretase modulator that reduces Aβ42 and Aβ40 secretion. The IC50s of CHF5074 for inhibition of COX-1 and COX-2 is above 100 μmol/L.
Targets
gamma-secretase [1]
In vitro
In vitro

In human neuroglioma cells over-expressing the Swedish mutated APP [human neuroglioma cell line expressing APPswe (H4swe)], CHF5074 preferentially lowers Aβ42 secretion with an IC50 of 3.6 µmol/L. CHF5074 does not display inhibitory activity on COX-1 and COX-2 enzymes when employed at concentrations up to 100 µmol/L and 300 µmol/L respectively[1].
In Vivo
In vivo

In rats, CHF5074 is orally well absorbed (50%) and is slowly eliminated from plasma (t1/2 ≈ 20 h). In Tg2576 transgenic mice, chronic treatment with CHF5074 markedly reduces brain Aβ burden without histological signs of peripheral Notch-mediated toxicity[1].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01602393 Completed
Alzheimer''s Disease
Chiesi Farmaceutici S.p.A.|Chiesi USA Inc.
 May 2012 Phase 2
NCT01421056 Completed
Alzheimer''s Disease
Chiesi Farmaceutici S.p.A.|Chiesi USA Inc.
 July 2011 Phase 2
NCT01258452 Completed
Alzheimer''s Disease
CERESPIR
 February 2011 Phase 1
NCT00954252 Completed
Alzheimer''s Disease
CERESPIR
 October 2009 Phase 1

Chemical Information & Solubility

Molecular Weight 325.16 Formula

C16H11Cl2FO2
CAS No. 749269-83-8 SDF --
Smiles C1CC1(C2=CC(=C(C=C2)C3=CC(=C(C=C3)Cl)Cl)F)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 65 mg/mL ( (199.9 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 12 mg/mL

Water : Insoluble


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In vivo
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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 ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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