2. Neuronal Signaling Stem Cell/Wnt Apoptosis
  3. γ-secretase Apoptosis
  4. Itanapraced

Itanapraced  (Synonyms: CHF5074; CSP-1103)

Cat. No.: HY-14399 Purity: 99.37%
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Itanapraced (CHF5074) is an orally active γ-secretase modulator and a non-steroidal anti-inflammatory derivative. Itanapraced reduces Aβ42 and Aβ40 secretion with IC50 values of 3.6 and 18.4 μM, respectively. Itanapraced inhibits cell apoptosis of hippocampal neurons induced by oxygen and glucose deprivation (OGD). Itanapraced can be used for the research of Alzheimer's disease.

For research use only. We do not sell to patients.

Itanapraced Chemical Structure

Itanapraced Chemical Structure

CAS No. : 749269-83-8

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10 mM * 1 mL in DMSO
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10 mg USD 140 In-stock
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Based on 1 publication(s) in Google Scholar

Itanapraced Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Itanapraced

  • Biological Activity

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Description

Itanapraced (CHF5074) is an orally active γ-secretase modulator and a non-steroidal anti-inflammatory derivative. Itanapraced reduces Aβ42 and Aβ40 secretion with IC50 values of 3.6 and 18.4 μM, respectively. Itanapraced inhibits cell apoptosis of hippocampal neurons induced by oxygen and glucose deprivation (OGD). Itanapraced can be used for the research of Alzheimer's disease[1][2].

IC50 & Target

IC50 value: 3.6 μM (Aβ42), 18.4 μM (Aβ40)[1]
In Vitro

Itanapraced (0.03-100 μM) inhibits Aβ secretion in human neuroglioma cells (H4swe) expressing APPswe with IC50 values of 3.6 and 18.4 μM for Aβ42 and Aβ40, respectively[1].
Itanapraced (5-200 μM) inhibits Notch processing in HEK293swe cells with concentrations over 15 μM[1].
Itanapraced (0-1000 μM; 30 min) dose-dependently inhibits the action potential with an IC50 value of 106 μM[2].
Itanapraced (30-100 μM) dose-dependently inhibits excitatory synaptic transmission[2].
Itanapraced (1-10 μM) significantly reduces cell apoptosis in hippocampal neurons induced by oxygen and glucose deprivation (OGD)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Itanapraced Related Antibodies
In Vivo

Itanapraced (oral administration; 375 ppm in the diet for 17 weeks) decreases Aβ42 and Aβ40 levels, and brain plaque burden in Tg2576 transgenic mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male and female Tg2576 transgenic mice expressing Swedish mutated form of human APP (APPswe)[1]
Dosage: 375 ppm
Administration: Oral administration; 375 ppm in the diet for 17 weeks
Result: Reduced total brain Aβ42 and Aβ40 levels, and brain plaque burden in aged Tg2576 mice. Caused no COX-mediated toxic effects in the gastrointestinal tract and Notch-mediated cell differentiation abnormalities in the ileum.
Clinical Trial
Molecular Weight

325.16

Formula

C16H11Cl2FO2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC(C1(CC1)C(C=C2)=CC(F)=C2C3=CC=C(Cl)C(Cl)=C3)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (307.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0754 mL 15.3770 mL 30.7541 mL
5 mM 0.6151 mL 3.0754 mL 6.1508 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (7.69 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.37%

COA (247 KB) HNMR (146 KB) RP-HPLC (248 KB) LCMS (259 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0754 mL 15.3770 mL 30.7541 mL 76.8852 mL
5 mM 0.6151 mL 3.0754 mL 6.1508 mL 15.3770 mL
10 mM 0.3075 mL 1.5377 mL 3.0754 mL 7.6885 mL
15 mM 0.2050 mL 1.0251 mL 2.0503 mL 5.1257 mL
20 mM 0.1538 mL 0.7689 mL 1.5377 mL 3.8443 mL
25 mM 0.1230 mL 0.6151 mL 1.2302 mL 3.0754 mL
30 mM 0.1025 mL 0.5126 mL 1.0251 mL 2.5628 mL
40 mM 0.0769 mL 0.3844 mL 0.7689 mL 1.9221 mL
50 mM 0.0615 mL 0.3075 mL 0.6151 mL 1.5377 mL
60 mM 0.0513 mL 0.2563 mL 0.5126 mL 1.2814 mL
80 mM 0.0384 mL 0.1922 mL 0.3844 mL 0.9611 mL
100 mM 0.0308 mL 0.1538 mL 0.3075 mL 0.7689 mL
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Itanapraced Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Itanapraced749269-83-8CHF5074 CSP-1103CHF 5074CHF-5074CSP1103CSP 1103CSP-1103γ-secretaseApoptosisGamma secretaseAβ42Aβ40Alzheimer's diseaseH4sweNotch processingapoptosisxcitatory synaptic transmissionInhibitorinhibitorinhibit

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