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Itanapraced (CHF 5074) Secretase modulator

Name: Itanapraced (CHF 5074)
Brand: Selleck Chemicals
SKU: S7323
Rating: 5 (1 reviews)

Cat.No.S7323

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.

Chemical Structure

Molecular Weight: 325.16

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Quality Control

Batch: Purity: 99.86%

99.86

Related Targets	HDAC Caspase Proteasome MMP HCV Protease Cysteine Protease DPP Tyrosinase HIV Protease Serine Protease
Other Secretase Inhibitors	DAPT RO4929097 (RG-4733) LY411575 Nirogacestat (PF-03084014) Dibenzazepine (YO-01027) Avagacestat (BMS-708163) Semagacestat (LY450139) MK-0752 MDL-28170 L-685,458

Chemical Information, Storage & Stability

Molecular Weight	325.16	Formula	C₁₆H₁₁Cl₂FO₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	749269-83-8	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	CSP-1103			Smiles	C1CC1(C2=CC(=C(C=C2)C3=CC(=C(C=C3)Cl)Cl)F)C(=O)O

Solubility

In vitro
Batch:

DMSO : 65 mg/mL (199.9 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 12 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	gamma-secretase
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.
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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/19239474/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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